CCT-245737

Based on 4 reference(s) in Google Scholar 8 10 4

Axon 3932

CAS [1489389-18-5]

MF C16H16F3N7O
MW 379.34

  • Purity: 99%
  • Optical purity: 99%
  • Soluble in DMSO

CCT-245737

Description

CCT-245737 is an orally active, potent and selective CHK1 inhibitor, with an enzaymatic IC50 value of 1.4 nM against CHK1 enzyme, and exhibited >1,000-fold selectivity against CHK2 and CDK1. It potently inhibited cellular CHK1 activity (IC50 30-220nM) 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 CCT-245737, causing increased DNA damage and apoptosis. CCT-245737 uniquely 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 CCT-245737. Finally, CCT-245737 also showed significant single-agent activity against a MYC-driven mouse model of B-cell lymphoma.

KEYWORDS: CCT-245737 | Supplier | CHK1 inhibitor | CCT245737 | CCT 245737 | PNT737 | PNT 737 | CT-CCT245 | CAS [1489389-18-5] | DNA-RNA | CHK | Inhibitor | Enzymes

Orally active, potent and selective CHK1 inhibitor

Chemical name

(R)-5-(4-(Morpholin-2-ylmethylamino)-5-(trifluoromethyl)pyridin-2-ylamino)pyrazine-2-carbonitrile

Source information

Sold in collaboration with Chemietek

Parent CAS No.

[1489389-18-5]

The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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