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CCT245737

Catalog No.: 16090101
Cas No.: 1489389-18-5
Purity : 98% by HNMR/HPLC 
16090101 - CCT245737 | CAS 1489389-18-5

Catalog number : 16090101

CAS number : 1489389-18-5

Molecular Formula : C16H16F3N7O 

Molecular Weight : 379.3 

Iupac Chemical Name : (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile 

Smile : N1C[C@@H](OCC1)CNC1=CC(=NC=C1C(F)(F)F)NC=1N=CC(=NC1)C#N

InChiKey : YBYYWUUUGCNAHQ-LLVKDONJSA-N

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SynonymsCCT245737;CCT 245737;CCT-245737 
Molecular FormulaC16H16F3N7O 
Molecular Weight379.3 
AppearanceSolid powder 
Purity98% by HNMR/HPLC 
SolubilitySoluble in DMSO, not in water 
Storage3 years -20ºCpowder 6 months-80ºCin solvent 
Shipping ConditionShipped under ambient temperature. 
SmileN1C[C@@H](OCC1)CNC1=CC(=NC=C1C(F)(F)F)NC=1N=CC(=NC1)C#N
InChiKeyYBYYWUUUGCNAHQ-LLVKDONJSA-N
InChiInChI=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
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CCT245737(CCT-245737, CAS 1489389-18-5) is the first orally active, clinical development candidate CHK1 inhibitor to be described. The IC50 was 1.4 nM against CHK1 enzyme and it exhibited>1,000-fold selectivity against CHK2 and CDK1. CCT245737 potently inhibited cellular CHK1 activity (IC50 30-220 nM) and enhanced gemcitabine and SN38 cytotoxicity in multiple human tumor cell lines and human tumor xenograft models. Mouse oral bioavailability was complete (100%) with extensive tumor exposure. Genotoxic-induced CHK1 activity (pS296 CHK1) and cell cycle arrest (pY15 CDK1) were inhibited both in vitro and in human tumor xenografts by CCT245737, causing increased DNA damage and apoptosis. Uniquely, we show CCT245737 enhanced gemcitabine antitumor activity to a greater degree than for higher doses of either agent alone, without increasing toxicity, indicating a true therapeutic advantage for this combination. Furthermore, development of a novel ELISA assay for pS296 CHK1 autophosphorylation, allowed the quantitative measurement of target inhibition in a RAS mutant human tumor xenograft of NSCLC at efficacious doses of CCT245737. Finally, CCT245737 also showed significant single-agent activity against a MYC-driven mouse model of B-cell lymphoma. In conclusion, CCT245737 is a new CHK1 inhibitor clinical development candidate scheduled for a first in man Phase I clinical trial, that will use the novel pS296 CHK1 ELISA to monitor target inhibition.

 

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