RON
Inhibitory Selectivity
RON 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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| S1124 |
BMS-754807BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met (c-Met), Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2. |
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| S2201 |
BMS-794833BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1. |
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| S1316 |
AMG-208AMG 208 is a highly selective dual c-Met and RON inhibitor with IC50 of 9 nM for c-Met. |
| 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%. |
|
| S1124 |
BMS-754807BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met (c-Met), Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2. |
|
|
| S2201 |
BMS-794833BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1. |
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| S1316 |
AMG-208AMG 208 is a highly selective dual c-Met and RON inhibitor with IC50 of 9 nM for c-Met. |
