CP-724714

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M.Wt: 469.53
Formula: C27H27N5O3
Solubility: Soluble to 10 mM in DMSO
Storage: Store at RT
Purity: 99%
CAS 383432-38-0

CP-724, 714 is an orally available, small molecule, potent HER-2 tyrosine kinase

inhibitor under development for the treatment of advanced HER2-overexpressing

cancers. It inhibits HER2-chimera phosphorylation with an IC50 of 15 ng/ ml ( 32 nM) ,

and is 500-fold selective for HER2 relative to other kinases ( e.g. EGFR, PDGFR, IGF-1R,

VEGFR-2, abl, src) . Antitumor activity of CP-724, 714 was observed in murine xenografts

of human adenocarcinomas of breast ( BT-474 and MDAMB-453) , pancreas

( Panc-1) , lung ( Calu-3) , and ovary ( SKOV-3) .Aditionally, CP-724, 714 showed a

favorable nonclinical toxicity profile with no apparent effects on cardiac tissue.

On the basis of these promising preclinical results, CP-724, 714 was advanced to

phase I clinical trials and is potentially another option for women with Her2-driven

breast cancer.

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