Tyro3
Inhibitory Selectivity
Tyro3 Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1561 |
BMS-777607BMS-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. |
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%. |
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| S7576 |
UNC2025 HClUNC2025 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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| S7638 |
LDC1267LDC1267 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. |
Time- and dose-dependent effects of LDC1267 in RSC96 cells.
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| S7325 |
UNC2881UNC2881 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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| 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. |
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| S9662New |
UNC2025UNC2025 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. |
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| S0071 |
RU-301RU-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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1561 |
BMS-777607BMS-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. |
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%. |
|
| S7576 |
UNC2025 HClUNC2025 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. |
||
| S7638 |
LDC1267LDC1267 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. |
Time- and dose-dependent effects of LDC1267 in RSC96 cells.
|
|
| S7325 |
UNC2881UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively. |
||
| 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. |
||
| S9662New |
UNC2025UNC2025 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. |
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| S0071 |
RU-301RU-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. |
