Information UNC2250 UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3. Targets Axl ; Axl ; Mer ; Tyro3 ; 1.7 nM; 100 nM In vitro UNC2250 efficiently inhibits Mer phosphorylation in 697 B-ALL cells and Colo699 NSCLC cells. Moreover, UNC2250 also displays functional antitumor activity by reducing colony-forming potential in both rhabdoid tumor cells and NSCLC cells. In vivo According to in vivo PK experiment, UNC2250 has a moderate half-life, clearance, and volume of distribution as well as reasonable oral bioavailability and good solubility. Cell Research(from reference) Cell lines：BT-12 rhabdoid tumor cells, and Colo699 NSCLC cells Concentrations：~3 μM for BT-12, ~300 nM for Colo699 Incubation Time：3 weeks for BT-12, 2 weeks for Colo699
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UNC2250
CAS number：1493694-70-4 molecular formula：C24H36N6O2
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| Chinese alias | 反式-4-[[2-(丁基氨基)-5-[5-(4-吗啉基甲基)-2-吡啶基]-4-嘧啶基]氨基]环己醇 | ||
| English alias | 4-[[2-(butylamino)-5-[5-(morpholin-4-ylmethyl)pyridin-2-yl]pyrimidin-4-yl]amino]cyclohexan-1-ol | ||
| CAS number | 1493694-70-4 | molecular formula | C24H36N6O2 |
| molecular weight | 440.58 g/mol | Exact mass | ≥99% |
| PSA | 95.400 Ų | logp | 2.800 |
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