FGFR

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1040	Sorafenib (BAY 43-9006) tosylate	0.01 mg/mL	127 mg/mL	'<1 mg/mL
S1490	Ponatinib (AP24534)	<1 mg/mL	30 mg/mL	<1 mg/mL
S2183	Infigratinib (BGJ398)	<1 mg/mL	1 mg/mL	<1 mg/mL
S1010	Nintedanib (BIBF 1120)	<1 mg/mL	6 mg/mL	3 mg/mL
S1035	Pazopanib HCl (GW786034 HCl)	<1 mg/mL	17 mg/mL	<1 mg/mL
S7647	Lucitanib (E3810) hydrochloride	59 mg/mL	59 mg/mL	'''30 mg/mL
S1264	PD173074	<1 mg/mL	100 mg/mL	100 mg/mL
S1018	Dovitinib (TKI-258)	<1 mg/mL	30 mg/mL	<1 mg/mL
S2801	AZD4547	<1 mg/mL	92 mg/mL	'<1 mg/mL
S1107	Danusertib (PHA-739358)	<1 mg/mL	95 mg/mL	<1 mg/mL
S1164	Lenvatinib (E7080)	<1 mg/mL	40 mg/mL	''<1 mg/mL
S1084	Brivanib (BMS-540215)	<1 mg/mL	74 mg/mL	3 mg/mL
S1181	ENMD-2076	1 mg/mL	105 mg/mL	<1 mg/mL
S3012	Pazopanib	<1 mg/mL	87 mg/mL	'<1 mg/mL
S2774	MK-2461	<1 mg/mL	99 mg/mL	'<1 mg/mL
S1138	Brivanib Alaninate (BMS-582664)	<1 mg/mL	88 mg/mL	'88 mg/mL
S8024	Tyrphostin AG 1296	<1 mg/mL	6 mg/mL	<1 mg/mL
S7167	SSR128129E	1 mg/mL	69 mg/mL	<1 mg/mL
S7057	LY2874455	<1 mg/mL	88 mg/mL	57 mg/mL
S8609	Derazantinib(ARQ-087)	<1 mg/mL	93 mg/mL	<1 mg/mL
S7667	SU5402	<1 mg/mL	59 mg/mL	<1 mg/mL
S7765	Dovitinib (TKI258) Lactate	66 mg/mL	100 mg/mL	'1 mg/mL
S8675	H3B-6527	<1 mg/mL	50 mg/mL	<1 mg/mL
S5240	Lenvatinib (E7080) Mesylate	-1 mg/mL	39 mg/mL	'''-1 mg/mL
S8882	ODM-203	<1 mg/mL	100 mg/mL	<1 mg/mL
S8401	Erdafitinib (JNJ-42756493)	<1 mg/mL	89 mg/mL	'89 mg/mL
S6539	ASP5878	<1 mg/mL	81 mg/mL	4 mg/mL
S8754	Alofanib (RPT835)	<1 mg/mL	83 mg/mL	'<1 mg/mL
S7940	NSC12	<1 mg/mL	96 mg/mL	'63 mg/mL
S6526	SKLB 610	<1 mg/mL	83 mg/mL	27 mg/mL
S8404	S49076	<1 mg/mL	87 mg/mL	'<1 mg/mL
S0088	Pemigatinib (INCB054828)	<1 mg/mL	40 mg/mL	'<1 mg/mL
S2300	Ferulic Acid	<1 mg/mL	39 mg/mL	39 mg/mL
S9031	Gambogenic acid	-1 mg/mL	100 mg/mL	-1 mg/mL
S8503	Fisogatinib (BLU-554)	<1 mg/mL	100 mg/mL	2 mg/mL
S8578	PRN1371	<1 mg/mL	100 mg/mL	6 mg/mL
S8161	ON123300	<1 mg/mL	29 mg/mL	'<1 mg/mL
S8493	PD-166866 (PD166866)	<1 mg/mL	14 mg/mL	3 mg/mL
S8965	BO-264	<1 mg/mL	71 mg/mL	<1 mg/mL
S8548	Roblitinib (FGF401)	<1 mg/mL	5 mg/mL	2 mg/mL
S8848	Futibatinib (TAS-120)	<1 mg/mL	84 mg/mL	<1 mg/mL
S7714	FIIN-2	<1 mg/mL	69 mg/mL	<1 mg/mL
S7665	Zoligratinib (Debio-1347)	<1 mg/mL	71 mg/mL	''1 mg/mL
S5234	Nintedanib Ethanesulfonate Salt	100 mg/mL	100 mg/mL	'5 mg/mL
S7819	BLU9931	<1 mg/mL	4 mg/mL	<1 mg/mL
S0487	Sulfatinib	˂1 mg/mL	96 mg/mL	''˂1 mg/mL
S8192	SUN11602	<1 mg/mL	90 mg/mL	31 mg/mL

亜型選択性的な製品

FGFR製品

All (47) FGFR阻害剤(46) FGFR活性剤(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1040	Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.	Cancer Cell, 2021, S1535-6108(21)00659-0 Leukemia, 2021, 10.1038/s41375-021-01308-z Theranostics, 2021, 11(12):5650-5674	Inhibition of breast cancer cell growth using sorafenib. MCF-7 breast cancer cells were treated with increasing concentrations of sorafenib for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells.
S1490	Ponatinib (AP24534) Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.	J Ethnopharmacol, 2022, 283:114667 Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Mol Syst Biol, 2021, 17(9):e10426	RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT.
S2183	Infigratinib (BGJ398) Infigratinib (BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.	Nature, 2021, 10.1038/s41586-020-03085-8 Nature, 2021, 595(7869):730-734 Cancer Cell, 2021, S1535-6108(21)00492-X	Anchorage-independent growth of NIN3T3 cells expressing FGFR2 fusions and its suppression by FGFR inhibitors (BGJ: BGJ398 and PD: PD173074). The percentage (+/- s.d.) of colonies formed in the presence of FGFR2 inhibitors (0.2 礛) and by KD mutants with respect to those formed by DMSO-treated cells are plotted at the bottom. The NIH3T3 clone expressing EZR-ROS1 was used as a negative control for FGFR inhibitors. *P<0.05.
S1010	Nintedanib (BIBF 1120) Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.	Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Cell Rep, 2021, 34(12):108882 Cancers (Basel), 2021, 13(16)4168	Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in "Materials and Methods". The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group
S1035	Pazopanib HCl (GW786034 HCl) Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.	Cancer Cell, 2021, S1535-6108(21)00659-0 Cancers (Basel), 2021, 13(14)3635 J Clin Endocrinol Metab, 2021, dgab020	Effect of HDIL-2/TKI on apoptosis of RCC cells. Three RCC cell lines treated with different concentrations of Pazopanib and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
S7647^新	Lucitanib (E3810) hydrochloride Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
S1264	PD173074 PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.	Adv Sci (Weinh), 2021, 8(2):2002922 Nat Commun, 2021, 12(1):3017 EMBO J, 2021, e107182	FGFR inhibitors block signaling in FGFR2-fusion-expressing cells. Activation of FGFR2 and MAPK by FGFR2-AHCYL1 and its suppression by FGFR inhibitors. Lysates from NIH3T3 cells expressing FGFR2-AHCYL1 or EZR-ROS1 (control) treated with vehicle (DMSO), 0.2 and 1 uM BGJ398, and 0.2 and 1 uM PD173074 were immunoblotted with the relevant antibodies. β-Actin was used as a loading control.
S1018	Dovitinib (TKI-258) Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.	Mol Cell, 2021, S1097-2765(21)00507-4 Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Cancer Res, 2021, canres.1780.2020	Orthotopic xenografts of HNSCC cell lines (A) SCC-1 and (B) OSC-19 were treated with dovitinib (20 mg/kg/day). In addition, the OSC-19 xenografts were treated with +/ radiation therapy. Marker, mean for triplicate; bars, SE. Statistical significance by unpaired t-test, p < 0.05.
S2801	AZD4547 AZD4547 (ABSK 091) is a novel selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM in cell-free assays, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38. Phase 2/3.	Nature, 2021, 595(7869):730-734 Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Sci Adv, 2021, 7(7)eabd2645	FCM evaluating lung CD11b+/Gr1+ myeloid cells isolated from 4T1 tumor-bearing mice after 20 days of treatment with AZD4547 or control. Statistical significance was assessed by unpaired t test.
S1107	Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.	Cancers (Basel), 2021, 13(6)1205 Life Sci Alliance, 2021, 4(8)e202101019 Mol Cell, 2020, 80(6):1104-1122.e9	Mice bearing subcutaneous allografts of conditional patched mutant tumor cells were treated twice weekly with vehicle (saline) or 30 mg/kg PHA-739358. (B)Images of tumors. (C) Tumor weights. Each point represents a single tumor, and grey lines represent mean tumor weights, which were significantly different between vehicle and PHA-739358 treated mice (p < 0.05, based on paired two-tailed t-test).
S1164	Lenvatinib (E7080) Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3.	Nature, 2021, 595(7869):730-734 Cancer Cell, 2021, S1535-6108(21)00659-0 Hepatology, 2021, 10.1002/hep.31921	Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.
S1084	Brivanib (BMS-540215) Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3.	J Cell Physiol, 2020, 235(2):1259-1273 Mol Pharm, 2019, 16(11):4436-4450 Eur J Cancer, 2016, 61:20-8	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of Brivanib by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
S1181	ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.	Cell, 2021, 184(2):334-351.e20 Sci Adv, 2021, 7(4)eabd7851 J Pediatr Hematol Oncol, 2019, 41(6):e359-e370	Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
S3012	Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.	Cancer Res, 2021, canres.1222.2021 Cancers (Basel), 2021, 13(14)3635 Radiother Oncol, 2021, 157:175-181	Three RCC cell lines treated with different concentrations of TKI and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
S2774	MK-2461 MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2. .	Mol Carcinog, 2021, 60(7):481-496 G3 (Bethesda), 2021, 11(10)jkab265 Mol Cell Biochem, 2018, 449(1-2):1-8	Both V-H cells and V-J cells are treated with MK-2461, XL-184 or ABT-869, respectively. (i-k) Western blot analysis of sFlt-1 expression after incubation with three VEGF-A receptor inhibitors or in the control.
S1138	Brivanib Alaninate (BMS-582664) Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.	Int J Oncol, 2014, 44(3):959-69 Assay Drug Dev Technol, 2014, 12(9-10):514-26
S8024	Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells.	J Cardiovasc Dev Dis, 2021, 8(3)28 Mol Med Rep, 2021, 23(4):1 CellPress, 2021, None	After inoculation with KAT4 cells, administration of compounds including MK-2206 (100 mg/kg), tyrphostin AG 1296 (100 mg/kg), or a combination of MK-2206 (100 mg/kg) and tyrphostin AG 1296 (100 mg/kg) was performed. The combination of MK-2206 and tyrphostin AG 1296 induced significant apoptosis of KAT4 tumor cells in vivo measured by the terminal deoxynucleotidyl transferase dUTP nick end labeling assay (green), and nuclei were stained with Hoechst (blue).
S7167	SSR128129E SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.	BMC Biol, 2021, 19(1):173 Front Oncol, 2021, 11:609918 Sci Rep, 2021, 11(1):6104	Western blot analysis of the expression and activation status (a) of pFGFR, pERK and Bim after treatment of API5-overexpressing cells (a) with either DMSO or SSR128129E.
S7057	LY2874455 LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.	Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118 Am J Cancer Res, 2020, 10(11):3765-3783 Protein Cell, 2019, 10(3):161-177	A: Overall structure of LY2874455/FGFR4 complex. B: The diagram of LY2874455. C: Fo-Fc omit map of LY2874455 in the FGFR4/LY2874455 complex. The electron density is superimposed with the final model. D: The DFG motif conformation of FGFR4. Active ApoFGFR4 DFG-in conformation is shown in blue (PDB: 4QQT); FGFR4/Ponatinib DFG-out conformation is shown in yellow (PDB: 4UXQ); FGFR4/BLU9931 DFG-in conformation is shown in pink (PDB: 4XCU); FGFR4/LY2874455 DFG-in conformation is shown in grey (this work). LY2874455 is highlighted in brown.
S8609	Derazantinib(ARQ-087) Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.
S7667	SU5402 SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.	Nature, 2021, 10.1038/s41586-020-03085-8 Nat Commun, 2021, 12(1):2551 Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118	Four FGFR inhibitors, namely PD-173074 (PD-74), PD-166866 (PD-66), SU5402 (SU54) and NVP-BGJ398 (BG-98), inhibit A673, SKNMC, POE, RDES and SKES Ewing cell growth in vitro in a dose-dependent manner, whereas normal cells (IMR90 fibroblasts) remained unaffected. PD-74 proved to be most effective in four out of five Ewing sarcoma cell lines tested. Cells were grown in 10% FBS conditions and cell proliferation was measured after 72 h using a Resazurin assay.
S7765	Dovitinib (TKI258) Lactate Dovitinib (TKI258, CHIR258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.	Mol Cell, 2021, S1097-2765(21)00507-4 Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Cancer Res, 2021, canres.1780.2020	(c) Percent survival for the AGS cancer cell line is shown with FGFR2 inhibitors of varying specificity. (d) The KatoIII diffuse gastric cancer cell line was treated with FGFR2 inhibitors of varying specificity. The Y-axis depicts percent survival versus the X-axis with log concentrations. In all panels, error bars represent standard error of the mean. The difference in percent cell survival between KatoIII and AGS cells was statistically significant (P <0.05) at the three highest concentrations of all drugs, except Brivanib which was only significant at the highest concentration.
S8675	H3B-6527 H3B-6527 is a highly selective covalent FGFR4 inhibitor with an IC50 value of <1.2 nM and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nM respectively).	J Exp Clin Cancer Res, 2021, 40(1):93 NPJ Precis Oncol, 2021, 5(1):66 Thorac Cancer, 2018, 9(12):1687-1698	KYSE150 and KYSE450 cells were treated each day with 1 μM H3B‐6527 or left untreated for three days, and lysates were immunoblotted with indicated antibodies. Western blotting demonstrated that the expression of EMT‐related markers (E‐cadherin, N‐cadherin, Claudin‐1, Vimentin, and Snail) was altered with FGFR4 blockade.
S5240	Lenvatinib (E7080) Mesylate Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.	J Immunother Cancer, 2021, 9(6)e002305 Cancer Lett, 2021, 519:46-62 Cancers (Basel), 2021, 13(11)2539
S8882	ODM-203 ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.
S8401	Erdafitinib (JNJ-42756493) Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.	Nature, 2021, 10.1038/s41586-020-03085-8 Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905	E, Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 μmol/L BGJ398 assessed by immunoblotting. FGFR inhibitors: AZD4547, BGJ398, and JNJ-42756493
S6539	ASP5878 ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively.	J Biol Chem, 2021, S0021-9258(21)00950-9 bioRxiv, 2020, 10.1101/2020.05.20.107326 bioRxiv, 2020, 10.1101/2020.05.20.107326
S8754	Alofanib (RPT835) Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.
S7940	NSC12 NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity.	Biomed Pharmacother, 2018, 107:359-367
S6526	SKLB 610 SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR.
S8404	S49076 S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.	Mol Brain, 2020, 4;13(1):66
S0088	Pemigatinib (INCB054828) Pemigatinib (INCB054828, Pemazyre) is an orally active and selective inhibitor of FGFR with IC50 of 0.4 nM, 0.5 nM, 1.2 nM and 30 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.	Cancer Res, 2021, canres.0955.2021 Cell Death Differ, 2021, 10.1038/s41418-021-00897-7 Cancer Med, 2021, 10.1002/cam4.4041
S2300	Ferulic Acid Ferulic Acid (Fumalic) is a hydroxycinnamic acid and a type of organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong. Ferulic acid is a novel fibroblast growth factor receptor (FGFR) inhibitor with IC50s of 3.78 μM and 12.5 μM for FGFR1 and FGFR2, respectively.	Biomed Pharmacother, 2019, 120:109482 J Med Virol, 2019, 91(8):1440-1447 J Nutr Biochem, 2015, 26(11):1379-84
S9031	Gambogenic acid Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.	Oncotarget, 2021, 12(6):549-561 Cancer Lett, 2020, 469:277-286
S8503	Fisogatinib (BLU-554) Fisogatinib (BLU-554) is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM.	Nature, 2021, 595(7869):730-734 Cancer Res, 2020, canres.1992.2020 Cancers (Basel), 2020, 12(8):E2010
S8578	PRN1371 PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively.	Nat Commun, 2021, 12(1):6572
S8161	ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.	J Cell Sci, 2021, jcs.258685 Molecules, 2020, 8;25(9) pii: E2220
S8493	PD-166866 (PD166866) PD-166866 is a synthetic molecule inhibiting the tyrosin kinase action of FGFR1, shows a very high selectivity towards FGFR1 and inhibits the auto-phosphorylation activity of FGRF1.	Cell Rep, 2021, 35(11):109233 Oxid Med Cell Longev, 2021, 2021:8996482 Histochem Cell Biol, 2021, 156(3):227-237
S8965	BO-264 BO-264 is a potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with IC50 of 188 nM and Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces SAC-dependent mitotic arrest, apoptosis and DNA damage with antitumor activities.
S8548	Roblitinib (FGF401) FGF401 is an FGFR4-selective inhibitor with an IC50 of 1.1 nM. It binds in a reversible covalent manner to the FGFR4 kinase domain and shows at least 1,000 fold selectivity against of panel of 65 kinases in biochemical assays.
S8848	Futibatinib (TAS-120) Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.	Cancer Res, 2021, canres.1780.2020 Oncogenesis, 2021, 10(7):55 Cancer Med, 2021, 10.1002/cam4.4041
S7714	FIIN-2 FIIN-2 is an irreversible, pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively.	Front Oncol, 2020, 10;10:331 Front Oncol, 2019, 9:179 Front Oncol, 2019, 9:179
S7665	Zoligratinib (Debio-1347) Zoligratinib (Debio-1347, CH5183284, FF284) is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.	J Cell Physiol, 2021, 10.1002/jcp.30657 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104 Elife, 2019, 8
S5234	Nintedanib Ethanesulfonate Salt Nintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively.	Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Cancers (Basel), 2021, 13(16)4168 Cell Death Dis, 2021, 12(10):947
S7819	BLU9931 BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.	Breast Cancer Res, 2021, 23(1):82 Aging (Albany NY), 2021, 13(2):2982-3009 Oncogene, 2020, 39(17):3507-3521	(E,G) Microscopic appearance of peritoneal dissemination of YTN16 (E) without BLU9931 and (G) with BLU9931 treatment for 3 weeks. (F,H) Microscopic features of s.c. tumor of YTN16 (F) without BLU9931 and (H) with BLU9931 treatment for 3 weeks. YTN16 tumor under treatment with BLU9931 does not form glandular structures.
S0487	Sulfatinib Sulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs.
S8192	SUN11602 SUN11602 is a small synthetic compound that mimics the neuroprotective activities of bFGF and activates key molecules in the FGF receptor-1-mitogen-activated protein kinase/extracellular signal-regulated kinase-1/2 kinase (FGFR-1-MEK/ERK) signaling pathway.

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S1040	Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.	Cancer Cell, 2021, S1535-6108(21)00659-0 Leukemia, 2021, 10.1038/s41375-021-01308-z Theranostics, 2021, 11(12):5650-5674	Inhibition of breast cancer cell growth using sorafenib. MCF-7 breast cancer cells were treated with increasing concentrations of sorafenib for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells.
S1490	Ponatinib (AP24534) Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.	J Ethnopharmacol, 2022, 283:114667 Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Mol Syst Biol, 2021, 17(9):e10426	RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT.
S2183	Infigratinib (BGJ398) Infigratinib (BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.	Nature, 2021, 10.1038/s41586-020-03085-8 Nature, 2021, 595(7869):730-734 Cancer Cell, 2021, S1535-6108(21)00492-X	Anchorage-independent growth of NIN3T3 cells expressing FGFR2 fusions and its suppression by FGFR inhibitors (BGJ: BGJ398 and PD: PD173074). The percentage (+/- s.d.) of colonies formed in the presence of FGFR2 inhibitors (0.2 礛) and by KD mutants with respect to those formed by DMSO-treated cells are plotted at the bottom. The NIH3T3 clone expressing EZR-ROS1 was used as a negative control for FGFR inhibitors. *P<0.05.
S1010	Nintedanib (BIBF 1120) Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.	Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Cell Rep, 2021, 34(12):108882 Cancers (Basel), 2021, 13(16)4168	Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in "Materials and Methods". The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group
S1035	Pazopanib HCl (GW786034 HCl) Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.	Cancer Cell, 2021, S1535-6108(21)00659-0 Cancers (Basel), 2021, 13(14)3635 J Clin Endocrinol Metab, 2021, dgab020	Effect of HDIL-2/TKI on apoptosis of RCC cells. Three RCC cell lines treated with different concentrations of Pazopanib and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
S7647^新	Lucitanib (E3810) hydrochloride Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
S1264	PD173074 PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.	Adv Sci (Weinh), 2021, 8(2):2002922 Nat Commun, 2021, 12(1):3017 EMBO J, 2021, e107182	FGFR inhibitors block signaling in FGFR2-fusion-expressing cells. Activation of FGFR2 and MAPK by FGFR2-AHCYL1 and its suppression by FGFR inhibitors. Lysates from NIH3T3 cells expressing FGFR2-AHCYL1 or EZR-ROS1 (control) treated with vehicle (DMSO), 0.2 and 1 uM BGJ398, and 0.2 and 1 uM PD173074 were immunoblotted with the relevant antibodies. β-Actin was used as a loading control.
S1018	Dovitinib (TKI-258) Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.	Mol Cell, 2021, S1097-2765(21)00507-4 Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Cancer Res, 2021, canres.1780.2020	Orthotopic xenografts of HNSCC cell lines (A) SCC-1 and (B) OSC-19 were treated with dovitinib (20 mg/kg/day). In addition, the OSC-19 xenografts were treated with +/ radiation therapy. Marker, mean for triplicate; bars, SE. Statistical significance by unpaired t-test, p < 0.05.
S2801	AZD4547 AZD4547 (ABSK 091) is a novel selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM in cell-free assays, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38. Phase 2/3.	Nature, 2021, 595(7869):730-734 Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Sci Adv, 2021, 7(7)eabd2645	FCM evaluating lung CD11b+/Gr1+ myeloid cells isolated from 4T1 tumor-bearing mice after 20 days of treatment with AZD4547 or control. Statistical significance was assessed by unpaired t test.
S1107	Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.	Cancers (Basel), 2021, 13(6)1205 Life Sci Alliance, 2021, 4(8)e202101019 Mol Cell, 2020, 80(6):1104-1122.e9	Mice bearing subcutaneous allografts of conditional patched mutant tumor cells were treated twice weekly with vehicle (saline) or 30 mg/kg PHA-739358. (B)Images of tumors. (C) Tumor weights. Each point represents a single tumor, and grey lines represent mean tumor weights, which were significantly different between vehicle and PHA-739358 treated mice (p < 0.05, based on paired two-tailed t-test).
S1164	Lenvatinib (E7080) Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3.	Nature, 2021, 595(7869):730-734 Cancer Cell, 2021, S1535-6108(21)00659-0 Hepatology, 2021, 10.1002/hep.31921	Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.
S1084	Brivanib (BMS-540215) Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3.	J Cell Physiol, 2020, 235(2):1259-1273 Mol Pharm, 2019, 16(11):4436-4450 Eur J Cancer, 2016, 61:20-8	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of Brivanib by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
S1181	ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.	Cell, 2021, 184(2):334-351.e20 Sci Adv, 2021, 7(4)eabd7851 J Pediatr Hematol Oncol, 2019, 41(6):e359-e370	Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
S3012	Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.	Cancer Res, 2021, canres.1222.2021 Cancers (Basel), 2021, 13(14)3635 Radiother Oncol, 2021, 157:175-181	Three RCC cell lines treated with different concentrations of TKI and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
S2774	MK-2461 MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2. .	Mol Carcinog, 2021, 60(7):481-496 G3 (Bethesda), 2021, 11(10)jkab265 Mol Cell Biochem, 2018, 449(1-2):1-8	Both V-H cells and V-J cells are treated with MK-2461, XL-184 or ABT-869, respectively. (i-k) Western blot analysis of sFlt-1 expression after incubation with three VEGF-A receptor inhibitors or in the control.
S1138	Brivanib Alaninate (BMS-582664) Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.	Int J Oncol, 2014, 44(3):959-69 Assay Drug Dev Technol, 2014, 12(9-10):514-26
S8024	Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells.	J Cardiovasc Dev Dis, 2021, 8(3)28 Mol Med Rep, 2021, 23(4):1 CellPress, 2021, None	After inoculation with KAT4 cells, administration of compounds including MK-2206 (100 mg/kg), tyrphostin AG 1296 (100 mg/kg), or a combination of MK-2206 (100 mg/kg) and tyrphostin AG 1296 (100 mg/kg) was performed. The combination of MK-2206 and tyrphostin AG 1296 induced significant apoptosis of KAT4 tumor cells in vivo measured by the terminal deoxynucleotidyl transferase dUTP nick end labeling assay (green), and nuclei were stained with Hoechst (blue).
S7167	SSR128129E SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.	BMC Biol, 2021, 19(1):173 Front Oncol, 2021, 11:609918 Sci Rep, 2021, 11(1):6104	Western blot analysis of the expression and activation status (a) of pFGFR, pERK and Bim after treatment of API5-overexpressing cells (a) with either DMSO or SSR128129E.
S7057	LY2874455 LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.	Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118 Am J Cancer Res, 2020, 10(11):3765-3783 Protein Cell, 2019, 10(3):161-177	A: Overall structure of LY2874455/FGFR4 complex. B: The diagram of LY2874455. C: Fo-Fc omit map of LY2874455 in the FGFR4/LY2874455 complex. The electron density is superimposed with the final model. D: The DFG motif conformation of FGFR4. Active ApoFGFR4 DFG-in conformation is shown in blue (PDB: 4QQT); FGFR4/Ponatinib DFG-out conformation is shown in yellow (PDB: 4UXQ); FGFR4/BLU9931 DFG-in conformation is shown in pink (PDB: 4XCU); FGFR4/LY2874455 DFG-in conformation is shown in grey (this work). LY2874455 is highlighted in brown.
S8609	Derazantinib(ARQ-087) Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.
S7667	SU5402 SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.	Nature, 2021, 10.1038/s41586-020-03085-8 Nat Commun, 2021, 12(1):2551 Proc Natl Acad Sci U S A, 2021, 118(20)e2100342118	Four FGFR inhibitors, namely PD-173074 (PD-74), PD-166866 (PD-66), SU5402 (SU54) and NVP-BGJ398 (BG-98), inhibit A673, SKNMC, POE, RDES and SKES Ewing cell growth in vitro in a dose-dependent manner, whereas normal cells (IMR90 fibroblasts) remained unaffected. PD-74 proved to be most effective in four out of five Ewing sarcoma cell lines tested. Cells were grown in 10% FBS conditions and cell proliferation was measured after 72 h using a Resazurin assay.
S7765	Dovitinib (TKI258) Lactate Dovitinib (TKI258, CHIR258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.	Mol Cell, 2021, S1097-2765(21)00507-4 Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Cancer Res, 2021, canres.1780.2020	(c) Percent survival for the AGS cancer cell line is shown with FGFR2 inhibitors of varying specificity. (d) The KatoIII diffuse gastric cancer cell line was treated with FGFR2 inhibitors of varying specificity. The Y-axis depicts percent survival versus the X-axis with log concentrations. In all panels, error bars represent standard error of the mean. The difference in percent cell survival between KatoIII and AGS cells was statistically significant (P <0.05) at the three highest concentrations of all drugs, except Brivanib which was only significant at the highest concentration.
S8675	H3B-6527 H3B-6527 is a highly selective covalent FGFR4 inhibitor with an IC50 value of <1.2 nM and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nM respectively).	J Exp Clin Cancer Res, 2021, 40(1):93 NPJ Precis Oncol, 2021, 5(1):66 Thorac Cancer, 2018, 9(12):1687-1698	KYSE150 and KYSE450 cells were treated each day with 1 μM H3B‐6527 or left untreated for three days, and lysates were immunoblotted with indicated antibodies. Western blotting demonstrated that the expression of EMT‐related markers (E‐cadherin, N‐cadherin, Claudin‐1, Vimentin, and Snail) was altered with FGFR4 blockade.
S5240	Lenvatinib (E7080) Mesylate Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.	J Immunother Cancer, 2021, 9(6)e002305 Cancer Lett, 2021, 519:46-62 Cancers (Basel), 2021, 13(11)2539
S8882	ODM-203 ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.
S8401	Erdafitinib (JNJ-42756493) Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.	Nature, 2021, 10.1038/s41586-020-03085-8 Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905	E, Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 μmol/L BGJ398 assessed by immunoblotting. FGFR inhibitors: AZD4547, BGJ398, and JNJ-42756493
S6539	ASP5878 ASP5878 is a novel FGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively.	J Biol Chem, 2021, S0021-9258(21)00950-9 bioRxiv, 2020, 10.1101/2020.05.20.107326 bioRxiv, 2020, 10.1101/2020.05.20.107326
S8754	Alofanib (RPT835) Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.
S7940	NSC12 NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity.	Biomed Pharmacother, 2018, 107:359-367
S6526	SKLB 610 SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR.
S8404	S49076 S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.	Mol Brain, 2020, 4;13(1):66
S0088	Pemigatinib (INCB054828) Pemigatinib (INCB054828, Pemazyre) is an orally active and selective inhibitor of FGFR with IC50 of 0.4 nM, 0.5 nM, 1.2 nM and 30 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.	Cancer Res, 2021, canres.0955.2021 Cell Death Differ, 2021, 10.1038/s41418-021-00897-7 Cancer Med, 2021, 10.1002/cam4.4041
S2300	Ferulic Acid Ferulic Acid (Fumalic) is a hydroxycinnamic acid and a type of organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong. Ferulic acid is a novel fibroblast growth factor receptor (FGFR) inhibitor with IC50s of 3.78 μM and 12.5 μM for FGFR1 and FGFR2, respectively.	Biomed Pharmacother, 2019, 120:109482 J Med Virol, 2019, 91(8):1440-1447 J Nutr Biochem, 2015, 26(11):1379-84
S9031	Gambogenic acid Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.	Oncotarget, 2021, 12(6):549-561 Cancer Lett, 2020, 469:277-286
S8503	Fisogatinib (BLU-554) Fisogatinib (BLU-554) is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM.	Nature, 2021, 595(7869):730-734 Cancer Res, 2020, canres.1992.2020 Cancers (Basel), 2020, 12(8):E2010
S8578	PRN1371 PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively.	Nat Commun, 2021, 12(1):6572
S8161	ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.	J Cell Sci, 2021, jcs.258685 Molecules, 2020, 8;25(9) pii: E2220
S8493	PD-166866 (PD166866) PD-166866 is a synthetic molecule inhibiting the tyrosin kinase action of FGFR1, shows a very high selectivity towards FGFR1 and inhibits the auto-phosphorylation activity of FGRF1.	Cell Rep, 2021, 35(11):109233 Oxid Med Cell Longev, 2021, 2021:8996482 Histochem Cell Biol, 2021, 156(3):227-237
S8965	BO-264 BO-264 is a potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with IC50 of 188 nM and Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces SAC-dependent mitotic arrest, apoptosis and DNA damage with antitumor activities.
S8548	Roblitinib (FGF401) FGF401 is an FGFR4-selective inhibitor with an IC50 of 1.1 nM. It binds in a reversible covalent manner to the FGFR4 kinase domain and shows at least 1,000 fold selectivity against of panel of 65 kinases in biochemical assays.
S8848	Futibatinib (TAS-120) Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.	Cancer Res, 2021, canres.1780.2020 Oncogenesis, 2021, 10(7):55 Cancer Med, 2021, 10.1002/cam4.4041
S7714	FIIN-2 FIIN-2 is an irreversible, pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively.	Front Oncol, 2020, 10;10:331 Front Oncol, 2019, 9:179 Front Oncol, 2019, 9:179
S7665	Zoligratinib (Debio-1347) Zoligratinib (Debio-1347, CH5183284, FF284) is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.	J Cell Physiol, 2021, 10.1002/jcp.30657 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104 Elife, 2019, 8
S5234	Nintedanib Ethanesulfonate Salt Nintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively.	Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x Cancers (Basel), 2021, 13(16)4168 Cell Death Dis, 2021, 12(10):947
S7819	BLU9931 BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.	Breast Cancer Res, 2021, 23(1):82 Aging (Albany NY), 2021, 13(2):2982-3009 Oncogene, 2020, 39(17):3507-3521	(E,G) Microscopic appearance of peritoneal dissemination of YTN16 (E) without BLU9931 and (G) with BLU9931 treatment for 3 weeks. (F,H) Microscopic features of s.c. tumor of YTN16 (F) without BLU9931 and (H) with BLU9931 treatment for 3 weeks. YTN16 tumor under treatment with BLU9931 does not form glandular structures.
S0487	Sulfatinib Sulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S8192	SUN11602 SUN11602 is a small synthetic compound that mimics the neuroprotective activities of bFGF and activates key molecules in the FGF receptor-1-mitogen-activated protein kinase/extracellular signal-regulated kinase-1/2 kinase (FGFR-1-MEK/ERK) signaling pathway.

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

S8192

SUN11602

SUN11602 is a small synthetic compound that mimics the neuroprotective activities of bFGF and activates key molecules in the FGF receptor-1-mitogen-activated protein kinase/extracellular signal-regulated kinase-1/2 kinase (FGFR-1-MEK/ERK) signaling pathway.