For research use only. Not for therapeutic Use.
CCT245737（Cat No.:I001831）, also known as SRA737 or PNT-737, is a potent orally active inhibitor of the checkpoint kinase 1 (CHK1). It exhibits an impressive IC50 value of 1.4 nM against CHK1. Notably, CCT245737 demonstrates a high selectivity for CHK1, being over 1000 times more potent against CHK1 compared to CHK2 and CDK1. As a CHK1 inhibitor, CCT245737 holds promise in cancer research and therapy, as CHK1 is involved in DNA damage response and cell cycle regulation, making it an attractive target for cancer treatment.
| Catalog Number | I001831 |
| CAS Number | 1489389-18-5 |
| Molecular Formula | C16H16F3N7O |
| Purity | ≥95% |
| Target | Checkpoint Kinase (Chk) |
| Solubility | DMSO ≥ 32 mg/mL |
| Storage | Store at -20°C |
| IUPAC Name | 5-[[4-[[(2R)-morpholin-2-yl]methylamino]-5-(trifluoromethyl)pyridin-2-yl]amino]pyrazine-2-carbonitrile |
| InChI | InChI=1S/C16H16F3N7O/c17-16(18,19)12-8-25-14(26-15-9-22-10(4-20)5-24-15)3-13(12)23-7-11-6-21-1-2-27-11/h3,5,8-9,11,21H,1-2,6-7H2,(H2,23,24,25,26)/t11-/m1/s1 |
| InChIKey | YBYYWUUUGCNAHQ-LLVKDONJSA-N |
| SMILES | C1COC(CN1)CNC2=CC(=NC=C2C(F)(F)F)NC3=NC=C(N=C3)C#N |
| Reference | </br>1: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). Osborne JD, Matthews TP, McHardy T, Proisy N, Cheung KM, Lainchbury M, Brown N, Walton MI, Eve PD, Boxall KJ, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Jamin Y, Robinson SP, Westwood IM, van Montfort RL, Leonard PM, Lamers MB, Reader JC, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I.J Med Chem. 2016 Jun 9;59(11):5221-37. doi: 10.1021/acs.jmedchem.5b01938. Epub 2016 May 23. PMID: 27167172 Free Article</br>2: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. Walton MI, Eve PD, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Boxall KJ, Tall M, Swales K, Matthews TP, McHardy T, Lainchbury M, Osborne J, Hunter JE, Perkins ND, Aherne GW, Reader JC, Raynaud FI, Eccles SA, Collins I, Garrett MD.Oncotarget. 2016 Jan 19;7(3):2329-42. doi: 10.18632/oncotarget.4919. PMID: 26295308 Free PMC Article |
