| Identification | Back Directory | [Name]
9H-Purin-6-amine, 2-(4-morpholinyl)-N-[(7-nitro-1H-benzimidazol-2-yl)methyl]-9-(3-thienyl)- | [CAS]
1446715-47-4 | [Synonyms]
SR-1277
9H-Purin-6-amine, 2-(4-morpholinyl)-N-[(7-nitro-1H-benzimidazol-2-yl)methyl]-9-(3-thienyl)- | [Molecular Formula]
C21H19N9O3S | [MOL File]
1446715-47-4.mol | [Molecular Weight]
477.5 |
| Hazard Information | Back Directory | [Description]
ML177 is a potent, selective and ATP competitive CK1δ/ε inhibitor. | [Uses]
SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer[1]. | [in vivo]
SR-1277 (1 mg/kg; i.v.) exhibits Cmax (1.2 μM), Cl (2.8 ml/min/kg), AUC(1.26 μM h), T1/2 (1.42 h) and brain penetration (24%) in mice[1]. | [IC 50]
CKIδ: 49 nM (IC50) | [References]
[1] Bibian M, et, al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80. DOI:10.1016/j.bmcl.2013.05.075 |
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