| 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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Int J Mol Sci, 2023, 10.3390/ijms242115903
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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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| S2841 |
Bemcentinib (R428)
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Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, demonstrating >100-fold selectivity for Axl over Abl. This compound is also more than 50- to 100-fold selective for Axl versus Mer and Tyro3, and exhibits 100-fold greater selectivity compared to InsR, EGFR, HER2, and PDGFRβ.
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Cell Stem Cell, 2025, S1934-5909(25)00265-6
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J Clin Invest, 2025, e180893
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Front Immunol, 2025, 16:1601420
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| 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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| S7754 |
ASP2215 (Gilteritinib)
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Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).
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J Adv Res, 2025, S2090-1232(25)00134-1
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Cancer Lett, 2025, 611:217446
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Mol Ther Nucleic Acids, 2025, 36(3):102611
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| E7462New |
Merestinib dihydrochloride
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Merestinib dihydrochloride (LY2801653 dihydrochloride) is an orally bioavailable, potent c-Met inhibitor exhibiting a Ki value of 2 nM. This compound demonstrates antitumor activity and inhibits multiple kinases, including MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM), and MKNK1/2 (IC50=7 nM).
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| S4001 |
Cabozantinib malate
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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. This compound induces apoptosis.
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Sci Rep, 2025, 15(1):35889
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bioRxiv, 2025, 2025.08.15.670608
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Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
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| S1561 |
BMS-777607
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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.
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Cell Rep, 2025, 44(8):116096
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Front Immunol, 2025, 16:1601420
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Endocrinology, 2025, 166(11)bqaf146
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| S8696 |
2-D08
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2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. This compound is a cell permeable, mechanistically unique inhibitor of protein sumoylation.
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Commun Biol, 2025, 8(1):1118
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Int Immunopharmacol, 2025, 149:114187
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Nat Commun, 2024, 15(1):9195
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| S7846 |
Dubermatinib(TP-0903)
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Dubermatinib (TP-0903) is a potent and selective AXL Inhibitor with IC50 of 27 nM, and it is highly effective in inducing apoptosis.
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Cancer Sci, 2025, 10.1111/cas.70151
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Biol Direct, 2025, 20(1):77
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Mol Oncol, 2024, 10.1002/1878-0261.13749
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