| S7067 |
Tepotinib
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Tepotinib is a potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. This compound induces autophagy. Phase 1.
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J Biomed Sci, 2025, 32(1):94
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Cell Oncol (Dordr), 2025, 10.1007/s13402-025-01097-y
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Lung Cancer, 2025, 201:108415
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| E4606 |
Dihexa
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Dihexa(PNB-0408), an oligopeptide drug, is an orally active and blood-brain barrier-permeable analog of angiotensin IV. It binds to hepatocyte growth factor (HGF) with high affinity and potentiates its activity at its receptor, c-Met. This compound can also be used as a therapeutic potential in the treatment of Alzheimer’s disease.
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| S1119 |
Cabozantinib (XL184)
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A potent VEGFR2 inhibitor with IC50 of 0.035 nM, Cabozantinib (XL184) also inhibits c-Met, Ret, 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. It induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.
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Nat Commun, 2025, 16(1):509
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Cell Death Differ, 2025, 10.1038/s41418-025-01510-x
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Cell Death Dis, 2025, 16(1):76
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| S9662 |
UNC2025
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UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. This compound 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.
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iScience, 2024, 27(7):110226
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Commun Biol, 2023, 6(1):916
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Commun Biol, 2023, 6(1):916
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| S1068 |
PF-02341066 (Crizotinib)
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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.
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Signal Transduct Target Ther, 2025, 10(1):124
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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Cell Death Differ, 2025, 10.1038/s41418-025-01510-x
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| S1112 |
SGX-523
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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.
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Stem Cell Res Ther, 2025, 16(1):526
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iScience, 2025, 28(2):111708
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Cancer Immunol Immunother, 2025, 74(2):58
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| S1111 |
Foretinib
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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.
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J Microbiol, 2025, 63(2):e2409001
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Int J Mol Sci, 2023, 24(1)757
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Biol Open, 2023, 12(8)bio059994
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| S1070 |
PHA-665752
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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.
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Cell Death Dis, 2025, 16(1):76
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Aging Cell, 2025, e70042.
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Biochim Biophys Acta Mol Cell Res, 2025, 1872(7):120001
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| S2788 |
Capmatinib (INC280)
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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.
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Mol Cancer, 2025, 24(1):272
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Cell Rep Med, 2025, 6(9):102335
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J Biomed Sci, 2025, 32(1):94
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| S5190 |
Crizotinib hydrochloride
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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.
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Cancer Discov, 2023, 13(3):598-615
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Nat Commun, 2023, 14(1):2829
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Cancer Res Commun, 2023, 3(4):659-671
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