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Tyro3 Products

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Catalog No. Product Name Information Product Use Citations Product Validations
S0071 RU-301 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.
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. Phase 1/2.
Elife, 2021, 10e63678
Oncogene, 2021, 10.1038/s41388-021-01869-4
Oncogene, 2021, 10.1038/s41388-021-02091-y
S7325 UNC2881 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.
Cell Rep, 2020, 30(11):3671-3681
Front Immunol, 2019, 10:2647
S7576 UNC2025 HCl 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.
Cell Rep, 2022, 38(13):110600
Cancers (Basel), 2021, 13(23)6072
Front Immunol, 2020, 11:564133
S7638 LDC1267 LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.
Cell Metab, 2021, S1550-4131(21)00326-0
J Clin Invest, 2021, 131(8)139434
Front Microbiol, 2020, 11:1292
S8570 RXDX-106 (CEP-40783) RXDX-106 (CEP-40783) 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.
J Oncol, 2022, 2022:2946929
Clin Cancer Res, 2021, 27(9):2533-2548
Cell Rep, 2021, 37(1):109789
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.
JCI Insight, 2022, 7(7)e154824
Front Immunol, 2020, 11:564133
Cell Signal, 2014, 26(1):149-61
S0071 RU-301 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.
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. Phase 1/2.
Elife, 2021, 10e63678
Oncogene, 2021, 10.1038/s41388-021-01869-4
Oncogene, 2021, 10.1038/s41388-021-02091-y
S7325 UNC2881 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.
Cell Rep, 2020, 30(11):3671-3681
Front Immunol, 2019, 10:2647
S7576 UNC2025 HCl 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.
Cell Rep, 2022, 38(13):110600
Cancers (Basel), 2021, 13(23)6072
Front Immunol, 2020, 11:564133
S7638 LDC1267 LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.
Cell Metab, 2021, S1550-4131(21)00326-0
J Clin Invest, 2021, 131(8)139434
Front Microbiol, 2020, 11:1292
S8570 RXDX-106 (CEP-40783) RXDX-106 (CEP-40783) 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.
J Oncol, 2022, 2022:2946929
Clin Cancer Res, 2021, 27(9):2533-2548
Cell Rep, 2021, 37(1):109789
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.
JCI Insight, 2022, 7(7)e154824
Front Immunol, 2020, 11:564133
Cell Signal, 2014, 26(1):149-61