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CP-724714HER2 inhibitor,potent and selective

CP-724714

Catalog No. A2412
Size Price Stock Qty
10mM (in 1mL DMSO) $99.00 In stock
5mg $85.00 In stock
25mg $320.00 In stock
100mg $800.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

CP-724714

Biological Activity

Description CP-724714 is an inhibitor of erbB2 and EGFR kinases with IC50 values of 10±3 nM and 6,400±2,100 nM, respectively.
Targets erbB2 EGFR        
IC50 10±3 nM 6,400±2,100 nM        

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Chemical Properties

Cas No. 537705-08-1 SDF Download SDF
Chemical Name 2-methoxy-N-[(E)-3-[4-[3-methyl-4-(6-methylpyridin-3-yl)oxyanilino]quinazolin-6-yl]prop-2-enyl]acetamide
Canonical SMILES CC1=NC=C(C=C1)OC2=C(C=C(C=C2)NC3=NC=NC4=C3C=C(C=C4)C=CCNC(=O)COC)C
Formula C27H27N5O3 M.Wt 469.53
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

CP-724714 is an inhibitor of erbB2 and EGFR kinases with IC50 values of 10±3 nmol/L and 6,400±2,100 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-erbB2

Xenografts. 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.