CP-724714

Short Summary : HER2 inhibitor,potent and selective

Category : JAK/STAT Signaling|EGFR

Purity : 0.98

CAS Number : 537705-08-1

Formula : C27H27N5O3

Molecular Weight : 469.53

SMILE : CC1=NC=C(C=C1)OC2=C(C=C(C=C2)NC3=NC=NC4=C3C=C(C=C4)C=CCNC(=O)COC)C

Solubility : >23.5mg/mL in DMSO

Storage : Store at -20°C

Description : CP-724714 is an inhibitor of erbB2 and EGFR kinases with IC50 values of 103 nmol/L and 6,4002,100 nmol/L, respectively [1].In the in vitro cell cycle assay, CP-724714 cause a G1 block of the Her2-amplified BT-474 breast cancer cells due to its inhibition of erbB2. CP-724714 at 1 mol/L can also reduce the level of phospho-erbB2 in these cells. In in vivo assay, CP-724714 cause a concentration-dependent reduction of tumor erbB2 receptor phosphorylation in athymic mice bearing FRE-erbB2Xenografts. CP-724714 treatments also resulted in a time- and dose-dependent induction of tumor cell apoptosis. In two human breast carcinoma models, BT-474 and MDA-MB-453, which are Her2 amplified and highly overexpress erbB2, CP-724714 is found to produce a dose-dependent inhibition of xenograft growth. In addition, CP-724,714 treatments induce reduction of downstream erbB2 RTK signaling. On the basis of these, CP-724,714 was advanced to phase I clinical trials and is potentially another option for Her2-driven breast cancer [1].References:[1] Jitesh P. Jani, Richard S. Finn, Mary Campbell, et al. Discovery and Pharmacologic Characterization of CP-724714, a Selective ErbB2 Tyrosine Kinase Inhibitor. Cancer Research. 2007 (67): 9887-9893.

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