CCT245737

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Chemical Structure| 1489389-18-5 同义名 : SRA737; PNT-737
CAS号 : 1489389-18-5
货号 : A433196
分子式 : C16H16F3N7O
纯度 : 97+%
分子量 : 379.34
MDL号 : MFCD30489721
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(79.08 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • Chk1

    Chk1, IC50:1.4 nM
描述 CCT245737, at a concentration of 10 µM, demonstrates significant inhibition (>80%) across a wide panel of 124 kinases, notably including ERK8, PKD1, RSK2, and RSK1, with IC50 values of 130, 298, 361, and 362 nM, respectively[1]. CCT245737 effectively disrupts the G2 checkpoint induced by VP-16 in various cell lines such as HT29, SW620, MiaPaCa-2, and Calu6, showcasing IC50 values ranging from 30 to 220 nM[2].
作用机制 CCT245737 binds in the ATP pocket of human CHK1. It is an ATP competitive inhibitor.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.18mL

2.64mL

1.32mL

26.36mL

5.27mL

2.64mL
参考文献

[1]Osborne JD, 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. 201

[2]Walton MI, 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 lymphoma.