cct245737-s-isomer

Description: CCT245737 S-enantiomer, the S-isomer of CCT245737, is a novel, potent, orally available and selective ATP-competitive inhibitor of CHK1 (checkpoint kinase 1) with an IC50 of 30-220 nM. It shows< 50% 10='' 121='' inhibition='' at='' m='' for='' representing='' a='' selectivity='' chk1='' of=''> 5000-fold over these enzymes. CCT245737 enhanced gemcitabine antitumor activity to a greater degree than for higher doses of either agent alone, without increasing toxicity. CCT2457374 shows an increase in plasma and tumoconcentrations between 3-100 mg/kg. CCT245737 has low predicted doses and exposures in humans which mitigated the residual weak in vitro hERG inhibition.

References: Oncotarget. 2016 Jan 19; 7(3):2329-42.

Related CAS#:1489389-18-5 (CCT245737)