CCT244747 is a novel potent, highly selective, orally active ATP-competitive CHK1 inhibitor with potential anticancer activity. CCT244747 inhibited cellular CHK1 activity (IC(50) 29-170 nmol/L), significantly enhanced the cytotoxicity of several anticancer drugs, and abrogated drug-induced S and G(2) arrest in multiple tumor cell lines. CCT244747 represents the first structural disclosure of a highly selective, orally active CHK1 inhibitor and warrants further evaluation alone or combined with genotoxic anticancer therapies.
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化学信息
名称 | CCT244747 |
Iupac 化学名称 | (R)-3-((1-(dimethylamino)propan-2-yl)oxy)-5-((4-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)amino)pyrazine-2-carbonitrile |
同义词 | CCT244747; CCT-244747; |
英文同义词 | CCT244747; CCT-244747; |
分子式 | C20H24N8O2 |
分子量 | 408.46 |
Smile | CN(C[C@@H](C)OC=1C(=NC=C(N1)NC1=NC=C(C(=C1)OC)C=1C=NN(C1)C)C#N)C |
InChiKey | IENLGMOXAQMNEH-CYBMUJFWSA-N |
InChi | InChI=1S/C20H24N8O2/c1-13(11-27(2)3)30-20-16(7-21)22-10-19(26-20)25-18-6-17(29-5)15(9-23-18)14-8-24-28(4)12-14/h6,8-10,12-13H,11H2,1-5H3,(H,23,25,26)/t13-/m1/s1 |
Cas号 | 1404095-34-6 |
相关CAS号 | |
外观性状 | Solid powder |
纯度 | 98% by HPLC |
存储 | -20 ºC for 3 years |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |