| 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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| E5942New |
UNC9426
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UNC9426 (compound 12) is a potent and orally bioavailable inhibitor of TYRO3 with an IC50 of 2.1 nM. It reduces platelet aggregation without prolonging bleeding time and effectively suppresses TYRO3-mediated signalling pathways in tumor cells and macrophages.
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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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| S7638 |
LDC1267
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LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. This compound displays lower activity against Met, Aurora B, Lck, Src, and CDK8.
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Cell Metab, 2021, S1550-4131(21)00326-0
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J Clin Invest, 2021, 131(8)e139434 139434
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J Clin Invest, 2021, 131(8)139434
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| S7576 |
UNC2025 HCl
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UNC2025 HCl is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
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Immunity, 2023, 56(8):1778-1793.e10
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Cell Rep, 2022, 38(13):110600
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Cancers (Basel), 2021, 13(23)6072
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| S8570 |
CEP-40783 (RXDX-106)
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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.
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UNIVERSITY OF CALIFORNIA, 2023,
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bioRxiv, 2023, 2023.10.20.563266
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Mol Cancer Res, 2022, 20(4):542-555
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| S7325 |
UNC2881
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UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively.
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Cell Rep, 2020, 30(11):3671-3681
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Front Immunol, 2019, 10:2647
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| S0071 |
RU-301
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RU-301 is a pan-TAM receptor (Axl, Tyro3 and Mertk) inhibitor that blocks the Axl receptor dimerization site with Kd of 12 μM and IC50 of 10 μM, respectively.
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