c-Met

c-Met製品

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  • c-Met阻害剤 (43)
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S1068 Crizotinib Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Nat Commun, 2024, 15(1):1009
Nat Commun, 2024, 15(1):51
Cancer Discov, 2023, 13(3):598-615
S1119 Cabozantinib (XL184) カボザンチニブ (Cabozantinib (XL184, BMS-907351)) は強力な VEGFR2 阻害剤であり、IC50 は 0.035 nM です。また c-Met, Ret, Kit, Flt-1/3/4, Tie2 および AXL に対しても阻害活性があり、cell-free assay における IC50 はそれぞれ 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM, 7 nM です。カボザンチニブは大腸がん細胞において AKT/GSK-3β/NF-κB 経路を介して PUMA 依存性アポトーシス (PUMA-dependent apoptosis) を誘発します。
Nat Cancer, 2023, 4(9):1345-1361
Mol Cell, 2023, 83(5):803-818.e8
Biomed Pharmacother, 2023, 164:115002
S1112 SGX-523 SGX-523 is a selective Met (c-Met) inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1.
PLoS Pathog, 2023, 19(8):e1011579
Pharmacol Res Perspect, 2023, 11(1):e01047
bioRxiv, 2023, 2023.02.23.529756
S4001 Cabozantinib malate Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Cancer Sci, 2023, 114(4):1651-1662
PLoS One, 2023, 18(2):e0277306
Adv Sci (Weinh), 2022, e2201478
S1111 Foretinib Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.
Int J Mol Sci, 2023, 24(1)757
Biol Open, 2023, 12(8)bio059994
Melanoma Res, 2023, 10.1097/CMR.0000000000000911
S1070 PHA-665752 PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM in cell-free assays, >50-fold selectivity for c-Met than RTKs or STKs.
Acta Neuropathol, 2024, 147(1):44
J Biol Chem, 2024, 300(3):105762
Int J Radiat Oncol Biol Phys, 2023, 116(3):640-654
S2788 Capmatinib Capmatinib is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1.
J Thorac Oncol, 2023, 10.1016/j.jtho.2023.10.017
J Exp Clin Cancer Res, 2023, 10.1186/s13046-023-02866-z
NPJ Precis Oncol, 2023, 7(1):107
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Cancer Discov, 2023, 13(3):598-615
Cancer Res Commun, 2023, 3(4):659-671
J Exp Clin Cancer Res, 2022, 41(1):309
S1080 SU11274 SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.
Cancer Cell Int, 2024, 24(1):43
J Transl Med, 2023, 21(1):530
J Transl Med, 2023, 21(1):530
S1561 BMS-777607 BMS-777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
Cancer Lett, 2024, 587:216692
Nat Commun, 2023, 14(1):4162
Oncogene, 2023, 42(21):1716-1727
S1114 JNJ-38877605 JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1.
Int J Mol Sci, 2023, 24(9)8086
Int J Mol Sci, 2023, 24(9)8086
Cancer Cell, 2022, S1535-6108(22)00312-9
S1124 BMS-754807 BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met (c-Met), Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.
Mol Neurodegener, 2023, 18(1):31
Cell Rep Med, 2023, 4(9):101162
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101285
S2753 Tivantinib Tivantinib is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Tivantinib (ARQ 197) induces a G2/M arrest and apoptosis.
Acta Neuropathol, 2024, 147(1):44
Elife, 2023, 12e79432
Cell Rep Med, 2022, 3(1):100492
S1094 PF-04217903 PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM in A549 cell line, susceptible to oncogenic mutations (no activity to Y1230C mutant). Phase 1.
Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.06.003
Neoplasia, 2019, 22(1):1-9
Sci Rep, 2019, 9(1):606
S1244 Amuvatinib (MP-470) Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2.
Microbiol Spectr, 2023, e0510522.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7674 Savolitinib (AZD6094) Savolitinib (Volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase.
Toxicol Appl Pharmacol, 2023, 475:116638
Sci Adv, 2023, 9(47):eadk1098
Exp Mol Med, 2022, 54(8):1225-1235
S1361 MGCD-265 analog MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
Protein Cell, 2019, 10(3):161-177
S2859 Golvatinib (E7050) Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.
Int J Mol Sci, 2023, 24(11)9606
Int J Mol Sci, 2022, 23(23)14884
Cancer Sci, 2020, 111(10):3813-3823
S7014 Merestinib (LY2801653) Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.
J Clin Invest, 2021, 131(11)146987
Mol Cancer Ther, 2021, molcanther.0344.2021
Cancer Commun (Lond), 2020, 11
S9662 UNC2025 UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.
Commun Biol, 2023, 6(1):916
Commun Biol, 2023, 6(1):916
Int J Mol Sci, 2023, 10.3390/ijms242115903
S8570 CEP-40783 (RXDX-106) CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.
Mol Cancer Res, 2022, 20(4):542-555
J Oncol, 2022, 2022:2946929
Clin Cancer Res, 2021, 27(9):2533-2548
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
S7669 NPS-1034 NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
Nat Commun, 2023, 14(1):4162
J Med Chem, 2021, 64(6):3165-3184
Sci Rep, 2021, 11(1):19667
S8167 AMG 337 AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the Met (c-Met) receptor with an IC50 of 1 nM.
J Biol Chem, 2022, S0021-9258(22)00070-9
Cancer Cell, 2019, 36(1):35-50
S3759 Norcantharidin Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
Phytother Res, 2023, 10.1002/ptr.7963
Front Pharmacol, 2022, 13:1019478
S6412 Altiratinib Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S5115 Sodium L-ascorbyl-2-phosphate Sodium L-ascorbyl-2-phosphate (Sodium ascorbyl monophosphate, Sodium ascorbyl phosphate, SAP) is specifically produced for use as a stabilized source of vitamin C in cosmetic products. It is used in skin care recipes for UV protection, collagen production, as an antioxidant and for its skin lightening and brightening effects.
Nature, 2022, 10.1038/s41586-022-04967-9
Stem Cell Res Ther, 2021, 12(1):48
S2201 BMS-794833 BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.
Cancer Res, 2021, canres.1428.2021
S2761 NVP-BVU972 NVP-BVU972 is a selective and potent Met (c-Met) inhibitor with IC50 of 14 nM.
PLoS Biol, 2021, 19(5):e3001263
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
S1316 AMG-208 AMG 208 is a highly selective dual c-Met and RON inhibitor with IC50 of 9 nM for c-Met.
S2747 AMG-458 AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells.
S6899 Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S0540 BAY-474 BAY-474 is an inhibitor of tyrosine-protein kinase c-Met and can act as an epigenetics probe.
S8854 JNJ-38877618(OMO-1) JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable Met (c-Met) kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant Met (c-Met) (2 and 3 nM IC50).
S9620 Elzovantinib (TPX-0022) Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.
S9308 Pulsatilla saponin D Pulsatilla saponin D (SB365), isolated from the root of Pulsatilla koreana, targets c-Met and exerts antiangiogenic and antitumor activities.
S6870 Ningetinib Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity.
S0361 AMG-1 AMG-1 (c-Met/RON Dual Kinase Inhibitor, RON-IN-1) is a potent inhibitor of human c-Met and RON with IC50 of 4 nM and 9 nM, respectively.
S6762 Bozitinib (PLB-1001) Bozitinib (PLB-1001, CBT-101, APL-101, CBI-3103) is a highly selective ATP-competitive c-Met inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) selectively inhibits MET-altered tumor cells in preclinical models.
S6764 Pamufetinib (TAS-115) Pamufetinib (TAS-115) is a highly potent c-Met and VEGFR dual inhibitor with IC50s of 30 nM and 32 nM for recombinant VEGFR2 and recombinant MET, respectively.
E2655 Terevalefim Terevalefim (ANG-3777), a small molecule hepatocyte growth factor (HGF) mimetic, induces c-MET dimerization and phosphorylation, reducing apoptosis and increasing cellular proliferation.
S7564 SAR125844 SAR125844 is a potent intravenously active and highly selective Met (c-Met) kinase inhibitor, displaying nanomolar activity against the wild-type kinase (IC50 value of 4.2 nmol/L) and H1094Y, Y1235D, M1250T, L1195V, and D1228H kinase domain mutants (IC50 values of 0.22, 1.7, 6.5, 65, and 81 nmol/L, respectively).
S8676 Glumetinib Glumetinib is a potent and highly selective c-Met inhibitor with an IC50 of 0.42 ± 0.02 nmol/L. Glumetinib has greater than 2,400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, and TyrO3.
D4046New Telisotuzumab vedotin Telisotuzumab vedotin (Teliso-V, ABBV-399) is an antibody-drug conjugate (ADC) composed of the anti–c-Met humanized monoclonal antibody coupled to the cytotoxic monomethyl auristatin E (MMAE) through a mc-val-cit-PABC type linker. Telisotuzumab vedotin can be used for research on advanced solid tumours.
E0142 XL092 XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.
S1068 Crizotinib Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Nat Commun, 2024, 15(1):1009
Nat Commun, 2024, 15(1):51
Cancer Discov, 2023, 13(3):598-615
S1119 Cabozantinib (XL184) カボザンチニブ (Cabozantinib (XL184, BMS-907351)) は強力な VEGFR2 阻害剤であり、IC50 は 0.035 nM です。また c-Met, Ret, Kit, Flt-1/3/4, Tie2 および AXL に対しても阻害活性があり、cell-free assay における IC50 はそれぞれ 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM, 7 nM です。カボザンチニブは大腸がん細胞において AKT/GSK-3β/NF-κB 経路を介して PUMA 依存性アポトーシス (PUMA-dependent apoptosis) を誘発します。
Nat Cancer, 2023, 4(9):1345-1361
Mol Cell, 2023, 83(5):803-818.e8
Biomed Pharmacother, 2023, 164:115002
S1112 SGX-523 SGX-523 is a selective Met (c-Met) inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1.
PLoS Pathog, 2023, 19(8):e1011579
Pharmacol Res Perspect, 2023, 11(1):e01047
bioRxiv, 2023, 2023.02.23.529756
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S4001 Cabozantinib malate Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Cancer Sci, 2023, 114(4):1651-1662
PLoS One, 2023, 18(2):e0277306
Adv Sci (Weinh), 2022, e2201478
S1111 Foretinib Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.
Int J Mol Sci, 2023, 24(1)757
Biol Open, 2023, 12(8)bio059994
Melanoma Res, 2023, 10.1097/CMR.0000000000000911
S1070 PHA-665752 PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM in cell-free assays, >50-fold selectivity for c-Met than RTKs or STKs.
Acta Neuropathol, 2024, 147(1):44
J Biol Chem, 2024, 300(3):105762
Int J Radiat Oncol Biol Phys, 2023, 116(3):640-654
S2788 Capmatinib Capmatinib is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1.
J Thorac Oncol, 2023, 10.1016/j.jtho.2023.10.017
J Exp Clin Cancer Res, 2023, 10.1186/s13046-023-02866-z
NPJ Precis Oncol, 2023, 7(1):107
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Cancer Discov, 2023, 13(3):598-615
Cancer Res Commun, 2023, 3(4):659-671
J Exp Clin Cancer Res, 2022, 41(1):309
S1080 SU11274 SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.
Cancer Cell Int, 2024, 24(1):43
J Transl Med, 2023, 21(1):530
J Transl Med, 2023, 21(1):530
S1561 BMS-777607 BMS-777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
Cancer Lett, 2024, 587:216692
Nat Commun, 2023, 14(1):4162
Oncogene, 2023, 42(21):1716-1727
S1114 JNJ-38877605 JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1.
Int J Mol Sci, 2023, 24(9)8086
Int J Mol Sci, 2023, 24(9)8086
Cancer Cell, 2022, S1535-6108(22)00312-9
S1124 BMS-754807 BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met (c-Met), Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.
Mol Neurodegener, 2023, 18(1):31
Cell Rep Med, 2023, 4(9):101162
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101285
S2753 Tivantinib Tivantinib is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Tivantinib (ARQ 197) induces a G2/M arrest and apoptosis.
Acta Neuropathol, 2024, 147(1):44
Elife, 2023, 12e79432
Cell Rep Med, 2022, 3(1):100492
S1094 PF-04217903 PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM in A549 cell line, susceptible to oncogenic mutations (no activity to Y1230C mutant). Phase 1.
Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.06.003
Neoplasia, 2019, 22(1):1-9
Sci Rep, 2019, 9(1):606
S1244 Amuvatinib (MP-470) Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2.
Microbiol Spectr, 2023, e0510522.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7674 Savolitinib (AZD6094) Savolitinib (Volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase.
Toxicol Appl Pharmacol, 2023, 475:116638
Sci Adv, 2023, 9(47):eadk1098
Exp Mol Med, 2022, 54(8):1225-1235
S1361 MGCD-265 analog MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
Protein Cell, 2019, 10(3):161-177
S2859 Golvatinib (E7050) Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.
Int J Mol Sci, 2023, 24(11)9606
Int J Mol Sci, 2022, 23(23)14884
Cancer Sci, 2020, 111(10):3813-3823
S7014 Merestinib (LY2801653) Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.
J Clin Invest, 2021, 131(11)146987
Mol Cancer Ther, 2021, molcanther.0344.2021
Cancer Commun (Lond), 2020, 11
S9662 UNC2025 UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.
Commun Biol, 2023, 6(1):916
Commun Biol, 2023, 6(1):916
Int J Mol Sci, 2023, 10.3390/ijms242115903
S8570 CEP-40783 (RXDX-106) CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.
Mol Cancer Res, 2022, 20(4):542-555
J Oncol, 2022, 2022:2946929
Clin Cancer Res, 2021, 27(9):2533-2548
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
S7669 NPS-1034 NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
Nat Commun, 2023, 14(1):4162
J Med Chem, 2021, 64(6):3165-3184
Sci Rep, 2021, 11(1):19667
S8167 AMG 337 AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the Met (c-Met) receptor with an IC50 of 1 nM.
J Biol Chem, 2022, S0021-9258(22)00070-9
Cancer Cell, 2019, 36(1):35-50
S3759 Norcantharidin Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
Phytother Res, 2023, 10.1002/ptr.7963
Front Pharmacol, 2022, 13:1019478
S6412 Altiratinib Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S2201 BMS-794833 BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.
Cancer Res, 2021, canres.1428.2021
S2761 NVP-BVU972 NVP-BVU972 is a selective and potent Met (c-Met) inhibitor with IC50 of 14 nM.
PLoS Biol, 2021, 19(5):e3001263
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
S1316 AMG-208 AMG 208 is a highly selective dual c-Met and RON inhibitor with IC50 of 9 nM for c-Met.
S2747 AMG-458 AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells.
S6899 Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S0540 BAY-474 BAY-474 is an inhibitor of tyrosine-protein kinase c-Met and can act as an epigenetics probe.
S8854 JNJ-38877618(OMO-1) JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable Met (c-Met) kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant Met (c-Met) (2 and 3 nM IC50).
S9620 Elzovantinib (TPX-0022) Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.
S9308 Pulsatilla saponin D Pulsatilla saponin D (SB365), isolated from the root of Pulsatilla koreana, targets c-Met and exerts antiangiogenic and antitumor activities.
S6870 Ningetinib Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity.
S0361 AMG-1 AMG-1 (c-Met/RON Dual Kinase Inhibitor, RON-IN-1) is a potent inhibitor of human c-Met and RON with IC50 of 4 nM and 9 nM, respectively.
S6762 Bozitinib (PLB-1001) Bozitinib (PLB-1001, CBT-101, APL-101, CBI-3103) is a highly selective ATP-competitive c-Met inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) selectively inhibits MET-altered tumor cells in preclinical models.
S6764 Pamufetinib (TAS-115) Pamufetinib (TAS-115) is a highly potent c-Met and VEGFR dual inhibitor with IC50s of 30 nM and 32 nM for recombinant VEGFR2 and recombinant MET, respectively.
S7564 SAR125844 SAR125844 is a potent intravenously active and highly selective Met (c-Met) kinase inhibitor, displaying nanomolar activity against the wild-type kinase (IC50 value of 4.2 nmol/L) and H1094Y, Y1235D, M1250T, L1195V, and D1228H kinase domain mutants (IC50 values of 0.22, 1.7, 6.5, 65, and 81 nmol/L, respectively).
S8676 Glumetinib Glumetinib is a potent and highly selective c-Met inhibitor with an IC50 of 0.42 ± 0.02 nmol/L. Glumetinib has greater than 2,400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, and TyrO3.
E0142 XL092 XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.
D4046New Telisotuzumab vedotin Telisotuzumab vedotin (Teliso-V, ABBV-399) is an antibody-drug conjugate (ADC) composed of the anti–c-Met humanized monoclonal antibody coupled to the cytotoxic monomethyl auristatin E (MMAE) through a mc-val-cit-PABC type linker. Telisotuzumab vedotin can be used for research on advanced solid tumours.

c-Met阻害剤の選択性比較

c-Metシグナル伝達経路

c-Metシグナル伝達経路
Tags: c-Met inhibition | c-Met cancer | c-Met pathway | c-Met activation | c-Met phosphorylation | c-Met inhibitor clinical trial | c-Met assay | c-Met inhibitor therapy | c-Met inhibitor review