Tyro3

Inhibitory Selectivity

Tyro3 Products

All (3) Tyro3 Inhibitors (3)

Catalog No.	Information	Product Use Citations	Product Validations
S1561	BMS-777607 BMS-777607 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.	Cell Metab, 2020, 4;31(2):406-421 e7 Front Oncol, 2020, 12;10:700 Cancer Commun (Lond), 2020, 11	Numbers of clonogenic cells from L3.6pl cells and CSCs^＋24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%.
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.	Mol Cell, 2019, 10.1016/j.molcel.2019.05.022 Am J Transl Res, 2019, 11(4):2288-2303 Am J Cancer Res, 2018, 8(8):1466-1482	Time- and dose-dependent effects of LDC1267 in RSC96 cells.
S8570	RXDX-106 (CEP-40783) RXDX-106 (CEP-40783) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/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 Clin Invest, 2018, 128(11):5034-5055

Catalog No.

Information

Product Use Citations

Product Validations

S1561

BMS-777607

BMS-777607 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.

Cell Metab, 2020, 4;31(2):406-421 e7

Front Oncol, 2020, 12;10:700

Cancer Commun (Lond), 2020, 11

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.

Mol Cell, 2019, 10.1016/j.molcel.2019.05.022

Am J Transl Res, 2019, 11(4):2288-2303

Am J Cancer Res, 2018, 8(8):1466-1482

S8570

RXDX-106 (CEP-40783)

RXDX-106 (CEP-40783) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/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 Clin Invest, 2018, 128(11):5034-5055

Catalog No.	Information	Product Use Citations	Product Validations
S1561	BMS-777607 BMS-777607 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.	Cell Metab, 2020, 4;31(2):406-421 e7 Front Oncol, 2020, 12;10:700 Cancer Commun (Lond), 2020, 11	Numbers of clonogenic cells from L3.6pl cells and CSCs^＋24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%.
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.	Mol Cell, 2019, 10.1016/j.molcel.2019.05.022 Am J Transl Res, 2019, 11(4):2288-2303 Am J Cancer Res, 2018, 8(8):1466-1482	Time- and dose-dependent effects of LDC1267 in RSC96 cells.
S8570	RXDX-106 (CEP-40783) RXDX-106 (CEP-40783) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/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 Clin Invest, 2018, 128(11):5034-5055

Catalog No.

Information

Product Use Citations

Product Validations

S1561