A selective HER2/ErbB2 tyrosine kinase inhibitor
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CP 724,714

Item No. 19172

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-methoxy-N-[(2E)-3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]-acetamide
CAS Number
383432-38-0
Molecular Formula
C27H27N5O3
Formula Weight
469.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 3 mg/mlEthanol: 2 mg/ml
λmax
243, 317, 347 nm
SMILES
O=C(COC)NC/C=C/C1=CC=C(N=CN=C2NC3=CC=C(OC4=CN=C(C)C=C4)C(C)=C3)C2=C1
InChi Code
InChI=1S/C27H27N5O3/c1-18-13-21(8-11-25(18)35-22-9-6-19(2)29-15-22)32-27-23-14-20(7-10-24(23)30-17-31-27)5-4-12-28-26(33)16-34-3/h4-11,13-15,17H,12,16H2,1-3H3,(H,28,33)(H,30,31,32)/b5-4+
InChi Key
LLVZBTWPGQVVLW-SNAWJCMRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    CP 724,714 is a selective inhibitor of HER2/ErbB2 with an IC50 value of 10 nM.1 It demonstrates greater than 640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, and c-Met.1 CP 724,714 has been shown to inhibit the proliferation of ErbB2-amplified cells, including BT474 and SK-BR-3 with IC50 values of 0.25 and 0.95 μM, respectively.1 It also demonstrates antitumor activity in various human tumor xenograft models.1 However, CP 724,714 was discontinued from clinical development due to hepatotoxicity caused by its ability to inhibit hepatic efflux transporters at low micromolar concentrations.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jani, J.P., Finn, R.S., Campbell, M., et al. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer Res. 67(20), 9887-9893 (2007).

    2. Feng, B., Xu, J.J., Bi, Y.A., et al. Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714. Toxicol. Sci. 108(2), 492-500 (2009).