UNC2250
UNC2250 is a highly selective inhibitor of Mer receptor tyrosine kinase with IC50 value of 1.7nM [1].
UNC2250 shows a potent inhibitory activity against Mer with IC50 value of 1.7nM. The IC50 values for other TAM kinases such as Axl and Tyro3 are 270nM and 100nM, respectively. In addition, UNC2250 shows no significant inhibition of a panel of 30 other kinases. In cell-based assays, UNC2250 inhibits the phosphorylation of Mer with IC50 value of 9.8nM in B-ALL cells. It also prevents the colony formation both in BT-12 cell lines and in Colo699 NSCLC cell lines. Furthermore, UNC2250 is proved to have a moderate half-life, clearance, distribution volume and good oral bioavailability [1].
References:
[1] Zhang W, Zhang D, Stashko M A, et al. Pseudo-Cyclization through Intramolecular Hydrogen Bond Enables Discovery of Pyridine Substituted Pyrimidines as New Mer Kinase Inhibitors. Journal of medicinal chemistry, 2013, 56(23): 9683-9692.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 440.58 |
| Cas No. | 1493694-70-4 |
| Formula | C24H36N6O2 |
| Solubility | ≥22.05 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 4-[[2-(butylamino)-5-[5-(morpholin-4-ylmethyl)pyridin-2-yl]pyrimidin-4-yl]amino]cyclohexan-1-ol |
| SDF | Download SDF |
| Canonical SMILES | CCCCNC1=NC=C(C(=N1)NC2CCC(CC2)O)C3=NC=C(C=C3)CN4CCOCC4 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | UNC2250 is a potent and selective inhibitor of Mer with an IC50 value of 1.7 nM. | |||||
| Targets | Mer | |||||
| IC50 | 1.7 nM | |||||
Quality Control & MSDS
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Chemical structure
