CCT245737
Cat. No.：YN290444
CAS No. ：1489389-18-5
| 产品名称: | CCT245737 |
| CAS No.: | 1489389-18-5 |
| Chemical Name: | 5-[[4-[[(2R)-2-morpholinylmethyl]amino]-5-(trifluoromethyl)-2-pyridinyl]amino]-2-pyrazinecarbonitrile |
| Synonyms: | ,SRA737 |
| 分子量: | 379.34 |
| 分子式: | C₁₆H₁₆F₃N₇O |
| SMILES: | FC(F)(F)C(C=NC(NC1=CN=C(C#N)C=N1)=C2)=C2NC[C@H]3CNCCO3 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | CCT245737 是一种可口服的，选择性的Chk1抑制剂，IC50值为 1.3 nM。 |
| IC50和靶点: | [{name:"Chk1:1.3 nM (IC50)"},{name: "Chk2:2440 nM (IC50)"},{name: "ERK8:130 nM (IC50)"},{name: "PKD1:298 nM (IC50)"},{name: "RSK2:361 nM (IC50)"},{name: "RSK1:362 nM (IC50)"},{name: "FLT3:582 nM (IC50)"},{name: "MARK3:698 nM (IC50)"},{name: "NUAK1:711 nM (IC50)"},{name: "CLK2:1370 nM (IC50)"},{name: "BRSK1:1660 nM (IC50)"},{name: "AMPK:2970 nM (IC50)"},{name: "PHK:3470 nM (IC50)"},{name: "CDK2/CyclA:3850 nM (IC50)"},{name: "CDK1/CyclB:9030 nM (IC50)"}] |
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Osborne, J.D., Matthews, T.P., McHardy, T., et al.Multiparameter lead optimization to give an oral checkpoint kinase 1 (CHK1) inhibitor clinical candidate: (R)-5-((4-((morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737)J. Med. Chem.59(11),5221-5237(2016)
Walton, M.I., P.D., E., Hayes, A., et al.The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphomaOncotarget7(3),2329-2342(2015)
