Bcr-Abl

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
S1021	Dasatinib	<1 mg/mL	98 mg/mL	<1 mg/mL
S1026	Imatinib Mesylate (STI571)	118 mg/mL	118 mg/mL	<1 mg/mL
S1490	Ponatinib (AP24534)	<1 mg/mL	30 mg/mL	<1 mg/mL
S1033	Nilotinib (AMN-107)	<1 mg/mL	27 mg/mL	<1 mg/mL
S1107	Danusertib (PHA-739358)	<1 mg/mL	95 mg/mL	<1 mg/mL
S2642	1-Naphthyl PP1(1-NA-PP1)	<1 mg/mL	9 mg/mL	<1 mg/mL
S1134	AT9283	<1 mg/mL	76 mg/mL	38 mg/mL
S2243	Degrasyn (WP1130)	<1 mg/mL	77 mg/mL	18 mg/mL
S1369	Bafetinib (INNO-406)	<1 mg/mL	100 mg/mL	<1 mg/mL
S2158	KW-2449	<1 mg/mL	67 mg/mL	67 mg/mL
S2202	NVP-BHG712	<1 mg/mL	101 mg/mL	3 mg/mL
S2622	PP121	<1 mg/mL	64 mg/mL	2 mg/mL
S2634	Rebastinib (DCC-2036)	<1 mg/mL	111 mg/mL	16 mg/mL
S7194	GZD824 Dimesylate	100 mg/mL	100 mg/mL	<1 mg/mL
S2899	GNF-2	<1 mg/mL	74 mg/mL	<1 mg/mL
S5254	Dasatinib hydrochloride	-1 mg/mL	100 mg/mL	-1 mg/mL
S5205	Nilotinib hydrochloride	-1 mg/mL	100 mg/mL	-1 mg/mL
S7782	Dasatinib Monohydrate	<1 mg/mL	21 mg/mL	<1 mg/mL
S8555	Asciminib (ABL001)	-1 mg/mL	89 mg/mL	89 mg/mL
S8134	Radotinib	<1 mg/mL	100 mg/mL	<1 mg/mL
S7269	PD173955	<1 mg/mL	15 mg/mL	<1 mg/mL
S8140	GNF-7	<1 mg/mL	20 mg/mL	<1 mg/mL
S7526	GNF-5	<1 mg/mL	83 mg/mL	20 mg/mL
S9141	Berbamine	-1 mg/mL	100 mg/mL	-1 mg/mL
S3609	Berbamine (dihydrochloride)	100 mg/mL	100 mg/mL	<1 mg/mL
S8888	GMB-475	<1 mg/mL	100 mg/mL	50 mg/mL

亜型選択性的な製品

Abl Selective

Bcr-Abl製品

All (26) Bcr-Abl阻害剤(25) Bcr-Abl化学物質(1) 新Bcr-Abl製品

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
S1021	Dasatinib Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.	Cell Rep, 2020, 30(3):793-806 Oncogene, 2020, 39(2):308-321 Oncogene, 2020, 10.1038/s41388-020-1255-y	Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.
S1026	Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.	Int J Mol Sci, 2020, 21(1) Nat Cell Biol, 2019, 21(6):778-790 Mol Cell, 2019, 75(2):252-266	THOC5 phospho-Y225 levels were assessed in the populations shown by flow cytometry following 24 h treatment with 5 μM imatinib, 150 nM dasatinib or 5 μM nilotinib. Results are displayed as mean fluorescence intensity (n= 4) ±s.e.m.
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.	Int J Cancer, 2020, 10.1002/ijc.32924 FASEB J, 2020, 34(3):3773-3791 Mol Cell Proteomics, 2020, 10.1074/mcp.RA119.001504	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.
S1033	Nilotinib (AMN-107) Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.	PLoS Pathog, 2020, 16(1):e1008261 FASEB J, 2020, 34(3):3773-3791 Commun Biol, 2020, 3(1):18	Effect of nilotinib on Bcr-Abl kinase activity in ABCB1- and ABCG2- overexpressing CD34⁺CD38^- cells. K562 parental cells and CD34⁺CD38^- subpopulation isolated from K562 cells were treated with nilotinib at 0.01, 0.1 and 1.0 umol/L for 12 h. Equal amount of protein was loaded for western blot analysis as described in the Experimental section. The experiments were repeated at least three times independently, and a representative experiment is shown.
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. Phase 2.	Toxicol Sci, 2019, 10.1093/toxsci/kfz123 Drug Deliv Transl Res, 2019, doi: 101007/s13346-019-00668-5 Leuk Lymphoma, 2019, 10.1080/10428194.2019.1594211	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).
S2642^新	1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively.
S1134	AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl(T315I). Phase 2.	J Pediatr Hematol Oncol, 2019, 41(6):e359-e370 J Clin Invest, 2018, 128(1):387-401 Nat Commun, 2018, 9(1):358	HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
S2243	Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).	J Biol Chem, 2020, 295(6):1694-1703 J Cell Biol, 2019, 218(7):2185-2197 J Biol Chem, 2019, 294(12):4572-4582	Protein expression by western blot analysis of cell lysates from MCF-7, TAM^R-4 and 164^R-7 cells treated for 3 days with vehicle (0.1% DMSO), 1 uM or 1.5 uM WP1130.
S1369	Bafetinib (INNO-406) Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2.	Drugs R D, 2019, 19(2):149-166 PLoS One, 2016, 11(10):e0164895 J Immunol, 2016, 197(5):1587-96	(A) The effect of bafetinib at 3 μM on the expression levels of ABCB1 in SW620/Ad300 cells for 24, 48 and 72 h. (B) The effect of bafetinib at 3 μM on the expression level of ABCG2 in NCI-H460/MX20 cells for 24, 48 and 72 h. Equal amounts of total cell lysate were used for each sample. The effect of bafetinib at 3 μM on the subcellular localization of ABCB1 in ABCB1-overexpressing (C) SW620/Ad300 cells and (D) HEK/ABCB1 cells for 24, 48 and 72 h. The effect of bafetinib at 3 μM on the subcellular localization of ABCG2 in ABCG2-overexpressing (E) NCI-H460/MX20 cells and (F) HEK/ABCG2-R482 cells. Scale bar, 10 μm. PI (propidium Iodide, red) counterstains the nuclei.
S2158	KW-2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.	Cell Rep, 2019, 28(9):2331-2344 Cell Chem Biol, 2018, 25(2):224-229 Mol Cancer Res, 2018, 16(10):1556-1567	Western blot analysis of p-histone and histone. 0-10μM KW2449 was added.
S2202	NVP-BHG712 NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.	Cancer Lett, 2020, 475:53-64 J Med Chem, 2019, 10.1021/acs.jmedchem.9b00855 Cell Death Dis, 2019, 10(11):801
S2622	PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.	PLoS One, 2016, 11(10):e0164895 Biochem Biophys Res Commun, 2015, 465(1):137-44 Tumour Biol, 2014, 35(9):8659-64	PP121 induces apoptosis in ATC cells. CAL62 cells were treated with PP121 at the indicated concentrations for 48 h, followed by PI staining. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown.
S2634	Rebastinib (DCC-2036) Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1.	Nat Cell Biol, 2019, 21(2):203-213 Int J Cancer, 2018, 10.1002/ijc.31915 Int J Mass Spectrom, 2018, 10.1016/j.ijms.2017.12.002	BaF3-T674I cells were exposed to the indicated concentrations of DCC-2036, imatinib or sorafenib for 36 h, the phosphorylated PDGFRα and total PDGFRα were analyzed by immunoblotting. Imatinib was used for comparison.
S7194	GZD824 Dimesylate GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.	J Leukoc Biol, 2019, 106(2):455-466 Oncotarget, 2017, 8(14):23213-23227 Sci Immunol, 2017, 2(10)	B. Western blot analysis of phosphorylated Akt, S6 and CrkL in T-ALL cell lines treated for 4 h with 2 μM Imatinib or Nilotinib or 0.1 μM GZD824. Twenty-five μg of protein were blotted to each lane. β-Actin documented equal lane loading. Imatinib, Nilotinib and GZD824 were abbreviated in IMA, NIL and GZD.
S2899	GNF-2 GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells.	J Gen Virol, 2018, 99(5):619-630 Cell Chem Biol, 2018, 25(2):206-214 JBMR Plus, 2018, 2(6):328-340	Cell viability of K562/IR cells and their parental cell lines after exposure to different concentrations of GNF-2 for 72 h.
S5254	Dasatinib hydrochloride Dasatinib hydrochloride is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.	Biomolecules, 2019, 9(11) Cancers (Basel), 2018, 10(12) Oncotarget, 2016, 7(37):59236-59244
S5205	Nilotinib hydrochloride Nilotinib hydrochloride is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.	Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007 Leuk Res, 2019, 78:3-11 Blood, 2018, 131(14):1532-1544
S7782	Dasatinib Monohydrate Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.	Front Microbiol, 2020, 10:2936 Nanomaterials (Basel), 2019, 9(9) Blood, 2018, 131(14):1532-1544	Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.
S8555	Asciminib (ABL001) Asciminib(ABL001) is a potent and selective allosteric ABL1 inhibitor with dissociation constant (Kd) of 0.5-0.8 nM and selectivity to the myristoyl pocket of ABL1.	J Leukoc Biol, 2019, 106(2):455-466 Proc Natl Acad Sci U S A, 2018, 115(46):11766-11771 Leukemia, 2017, 31(11):2376-2387	Co-immunoprecipitation assays of UT7 BCR–ABL T315I (UT7 B/A T315I) cells with or without ponatinib (20 nm) or ABL001 (4 μm) treatment for 24 h. All protein extracts were immunoprecipitated with an anti-DNM2 antibody and immunoblotted with a pan-anti-p-Tyr antibody (4G10).
S8134	Radotinib Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.	Drugs R D, 2019, 19(2):149-166
S7269	PD173955 PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM.
S8140	GNF-7 GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively.
S7526	GNF-5 GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.	J Gen Virol, 2018, 99(5):619-630 Leukemia, 2017, 31(5):1096-1107 Oncogene, 2017, 36(32):4585-4596	IC50 values for GNF-5-treated Ba/F3 cells expressing BCR-ABL1 or ABL1 1b mutants (a) described to confer ABL001 resistance in BCR-ABL1, (b) identified by mutagenesis screen. after 48 hours. Error bars represent SD of triplicates from three independent experiments. Significance levels in comparison with BCR-ABL1 are indicated (NS, not significant; P<0.05, P<0.01, **P<0.001, two-tailed unpaired t-test).
S9141	Berbamine Berbamine (BA), a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB.	Onco Targets Ther, 2019, 12:11437-11451
S3609	Berbamine (dihydrochloride) Berbamine (BBM) is a natural bisbenzylisoquinoline product isolated from traditional Chinese herbal medicine Berberis amurensis. It is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB.
S8888^新	GMB-475 GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.

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
S1021	Dasatinib Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.	Cell Rep, 2020, 30(3):793-806 Oncogene, 2020, 39(2):308-321 Oncogene, 2020, 10.1038/s41388-020-1255-y	Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.
S1026	Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.	Int J Mol Sci, 2020, 21(1) Nat Cell Biol, 2019, 21(6):778-790 Mol Cell, 2019, 75(2):252-266	THOC5 phospho-Y225 levels were assessed in the populations shown by flow cytometry following 24 h treatment with 5 μM imatinib, 150 nM dasatinib or 5 μM nilotinib. Results are displayed as mean fluorescence intensity (n= 4) ±s.e.m.
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.	Int J Cancer, 2020, 10.1002/ijc.32924 FASEB J, 2020, 34(3):3773-3791 Mol Cell Proteomics, 2020, 10.1074/mcp.RA119.001504	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.
S1033	Nilotinib (AMN-107) Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.	PLoS Pathog, 2020, 16(1):e1008261 FASEB J, 2020, 34(3):3773-3791 Commun Biol, 2020, 3(1):18	Effect of nilotinib on Bcr-Abl kinase activity in ABCB1- and ABCG2- overexpressing CD34⁺CD38^- cells. K562 parental cells and CD34⁺CD38^- subpopulation isolated from K562 cells were treated with nilotinib at 0.01, 0.1 and 1.0 umol/L for 12 h. Equal amount of protein was loaded for western blot analysis as described in the Experimental section. The experiments were repeated at least three times independently, and a representative experiment is shown.
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. Phase 2.	Toxicol Sci, 2019, 10.1093/toxsci/kfz123 Drug Deliv Transl Res, 2019, doi: 101007/s13346-019-00668-5 Leuk Lymphoma, 2019, 10.1080/10428194.2019.1594211	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).
S2642^新	1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively.
S1134	AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl(T315I). Phase 2.	J Pediatr Hematol Oncol, 2019, 41(6):e359-e370 J Clin Invest, 2018, 128(1):387-401 Nat Commun, 2018, 9(1):358	HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
S2243	Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).	J Biol Chem, 2020, 295(6):1694-1703 J Cell Biol, 2019, 218(7):2185-2197 J Biol Chem, 2019, 294(12):4572-4582	Protein expression by western blot analysis of cell lysates from MCF-7, TAM^R-4 and 164^R-7 cells treated for 3 days with vehicle (0.1% DMSO), 1 uM or 1.5 uM WP1130.
S1369	Bafetinib (INNO-406) Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2.	Drugs R D, 2019, 19(2):149-166 PLoS One, 2016, 11(10):e0164895 J Immunol, 2016, 197(5):1587-96	(A) The effect of bafetinib at 3 μM on the expression levels of ABCB1 in SW620/Ad300 cells for 24, 48 and 72 h. (B) The effect of bafetinib at 3 μM on the expression level of ABCG2 in NCI-H460/MX20 cells for 24, 48 and 72 h. Equal amounts of total cell lysate were used for each sample. The effect of bafetinib at 3 μM on the subcellular localization of ABCB1 in ABCB1-overexpressing (C) SW620/Ad300 cells and (D) HEK/ABCB1 cells for 24, 48 and 72 h. The effect of bafetinib at 3 μM on the subcellular localization of ABCG2 in ABCG2-overexpressing (E) NCI-H460/MX20 cells and (F) HEK/ABCG2-R482 cells. Scale bar, 10 μm. PI (propidium Iodide, red) counterstains the nuclei.
S2158	KW-2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.	Cell Rep, 2019, 28(9):2331-2344 Cell Chem Biol, 2018, 25(2):224-229 Mol Cancer Res, 2018, 16(10):1556-1567	Western blot analysis of p-histone and histone. 0-10μM KW2449 was added.
S2202	NVP-BHG712 NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.	Cancer Lett, 2020, 475:53-64 J Med Chem, 2019, 10.1021/acs.jmedchem.9b00855 Cell Death Dis, 2019, 10(11):801
S2622	PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.	PLoS One, 2016, 11(10):e0164895 Biochem Biophys Res Commun, 2015, 465(1):137-44 Tumour Biol, 2014, 35(9):8659-64	PP121 induces apoptosis in ATC cells. CAL62 cells were treated with PP121 at the indicated concentrations for 48 h, followed by PI staining. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown.
S2634	Rebastinib (DCC-2036) Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1.	Nat Cell Biol, 2019, 21(2):203-213 Int J Cancer, 2018, 10.1002/ijc.31915 Int J Mass Spectrom, 2018, 10.1016/j.ijms.2017.12.002	BaF3-T674I cells were exposed to the indicated concentrations of DCC-2036, imatinib or sorafenib for 36 h, the phosphorylated PDGFRα and total PDGFRα were analyzed by immunoblotting. Imatinib was used for comparison.
S7194	GZD824 Dimesylate GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.	J Leukoc Biol, 2019, 106(2):455-466 Oncotarget, 2017, 8(14):23213-23227 Sci Immunol, 2017, 2(10)	B. Western blot analysis of phosphorylated Akt, S6 and CrkL in T-ALL cell lines treated for 4 h with 2 μM Imatinib or Nilotinib or 0.1 μM GZD824. Twenty-five μg of protein were blotted to each lane. β-Actin documented equal lane loading. Imatinib, Nilotinib and GZD824 were abbreviated in IMA, NIL and GZD.
S2899	GNF-2 GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells.	J Gen Virol, 2018, 99(5):619-630 Cell Chem Biol, 2018, 25(2):206-214 JBMR Plus, 2018, 2(6):328-340	Cell viability of K562/IR cells and their parental cell lines after exposure to different concentrations of GNF-2 for 72 h.
S5254	Dasatinib hydrochloride Dasatinib hydrochloride is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.	Biomolecules, 2019, 9(11) Cancers (Basel), 2018, 10(12) Oncotarget, 2016, 7(37):59236-59244
S5205	Nilotinib hydrochloride Nilotinib hydrochloride is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.	Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007 Leuk Res, 2019, 78:3-11 Blood, 2018, 131(14):1532-1544
S7782	Dasatinib Monohydrate Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.	Front Microbiol, 2020, 10:2936 Nanomaterials (Basel), 2019, 9(9) Blood, 2018, 131(14):1532-1544	Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.
S8555	Asciminib (ABL001) Asciminib(ABL001) is a potent and selective allosteric ABL1 inhibitor with dissociation constant (Kd) of 0.5-0.8 nM and selectivity to the myristoyl pocket of ABL1.	J Leukoc Biol, 2019, 106(2):455-466 Proc Natl Acad Sci U S A, 2018, 115(46):11766-11771 Leukemia, 2017, 31(11):2376-2387	Co-immunoprecipitation assays of UT7 BCR–ABL T315I (UT7 B/A T315I) cells with or without ponatinib (20 nm) or ABL001 (4 μm) treatment for 24 h. All protein extracts were immunoprecipitated with an anti-DNM2 antibody and immunoblotted with a pan-anti-p-Tyr antibody (4G10).
S8134	Radotinib Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.	Drugs R D, 2019, 19(2):149-166
S7269	PD173955 PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM.
S8140	GNF-7 GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively.
S7526	GNF-5 GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.	J Gen Virol, 2018, 99(5):619-630 Leukemia, 2017, 31(5):1096-1107 Oncogene, 2017, 36(32):4585-4596	IC50 values for GNF-5-treated Ba/F3 cells expressing BCR-ABL1 or ABL1 1b mutants (a) described to confer ABL001 resistance in BCR-ABL1, (b) identified by mutagenesis screen. after 48 hours. Error bars represent SD of triplicates from three independent experiments. Significance levels in comparison with BCR-ABL1 are indicated (NS, not significant; P<0.05, P<0.01, **P<0.001, two-tailed unpaired t-test).
S9141	Berbamine Berbamine (BA), a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB.	Onco Targets Ther, 2019, 12:11437-11451
S3609	Berbamine (dihydrochloride) Berbamine (BBM) is a natural bisbenzylisoquinoline product isolated from traditional Chinese herbal medicine Berberis amurensis. It is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB.

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S8888^新	GMB-475 GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.

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S8888^新

GMB-475

GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.