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CP-724714 | HER2 inhibitor

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Price:
$119.00
Catalog #:
C2772-5
Quantity:


Product Description

CP-724714 is a quinazoline-based, orally-available, ATP-competitive inhibitor of erbB2 at an IC50 of 10 nM, with exquisite selectivity over EGFR kinase (6.4 uM) and >1000-fold selectivity over IR, IGFR, PDGFRb, VEGFR2, Abl, Src, cMet, JNK, CDK2, and CDK5. [1] CP-724714 is a potent inhibitor of erbB2 autophosphorylation (EC50 = 1 ug/mL) and induces G1 cell cycle arrest with concomitant reduction in S-phase cells. [1]

CP-724714 exhibits linear single-dose and multiple-dose pharmacokinetics. [2], but was discontinued from clinical development due to unexpected hepatotoxicity. [3]


Technical information:

Chemical Formula:   C27H27N5O3
CAS #:   383432-38-0
Molecular Weight:   469.53
Purity:   > 99%
Appearance:   White
Chemical Name:   (E)-2-methoxy-N-(3-(4-(3-methyl-4-(6-methylpyridin-3-yloxy)phenylamino)quinazolin-6-yl)allyl)acetamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   CP-724714, CP724714, 383432-38-0

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Jani et al., Discovery and Pharmacologic Characterization of CP-724714, a Selective ErbB2 Tyrosine Kinase Inhibitor. Cancer Res. 2007, 67, 9887-9893. Pubmed ID: 17942920
2. Guo et al., Pharmacokinetics of a HER2 tyrosine kinase inhibitor CP-724,714 in patients with advanced malignant HER2 positive solid tumors: correlations with clinical characteristics and safety. Cancer Chemother. Pharmacol., 2008, 62, 97-109. Pubmed ID: 17805538
3. Feng et al., Role of Hepatic Transporters in the Disposition and Hepatotoxicity of a HER2 Tyrosine Kinase Inhibitor CP-724,714. Toxicol. Sci. 2009, 108(2), 492-500.

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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