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CP-724714

Catalog No. T4014   CAS 383432-38-0
Synonyms: CP724714, CP 724714

CP-724714 (CP724714) is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), <640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc.

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CP-724714 Chemical Structure
CP-724714, CAS 383432-38-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
2 mg In stock $ 53.00
5 mg In stock $ 87.00
10 mg In stock $ 159.00
25 mg In stock $ 287.00
50 mg In stock $ 477.00
100 mg In stock $ 695.00
1 mL * 10 mM (in DMSO) In stock $ 91.00
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Purity: 99.1%
Purity: 98.82%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CP-724714 (CP724714) is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), >640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc.
Targets&IC50 HER2:10 nM, ErbB2:10 nM
In vitro CP-724714 is obvious selectively against EGFR (IC50: 6.4 μM). CP-724714 is >1,000-fold less potent for IGF-1R, IR, VGFR2, PDGFRβ, Src, ZAP-70, JNK-2/3, and CDK-2/5. CP-724714 markedly reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain (IC50: 32 nM). CP-724714 inhibits the proliferation of erbB2-amplified cells including BT-474 (IC50: 0.25 μM) and SKBR3 (IC50: 0.95 μM). CP-724714 (1 μM) induces the accumulation of cells in G1 phase and a marked reduction in S-phase in BT-474 cells. CP-724714 inhibits TC transport in membrane vesicles expressing human bile salt export pump (IC50: 16 μM) and inhibits the major efflux transporter in bile canaliculi, MDR1 (IC50: 28 μM).
In vivo CP-724714 (25 mg/kg) is rapidly absorbed after p.o. administration and causes reduction of tumor erbB2 receptor phosphorylation after dosing in FRE-erbB2 or BT-474 xenografts. CP-724,714 induces apoptosis in FRE-erbB2 xenograft-bearing (s.c.) mice and shows 50% tumor growth inhibition at 50 mg/kg, without mortality or weight loss. In MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts, CP-724714 also has great antitumor activity. In BT-474 xenografts, CP-724714 (30/100 mg/kg) reduces the extracellular signal-regulated kinase and Akt phosphorylation.
Synonyms CP724714, CP 724714
Molecular Weight 469.54
Formula C27H27N5O3
CAS No. 383432-38-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (117.14 mM)

TargetMolReferences and Literature

1. Jani JP, et al. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer Res, 2007, 67(20), 9887-9893. 2. Feng B, 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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Membrane Protein-targeted Compound Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Bioactive Compound Library Immuno-Oncology Compound Library Anti-Breast Cancer Compound Library Anti-Liver Cancer Compound Library Anti-Prostate Cancer Compound Library

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Keywords

CP-724714 383432-38-0 Angiogenesis Apoptosis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR mice CP724714 Epidermal growth factor receptor autophosphorylation athymic inhibit cycle HER1 ErbB-1 Inhibitor oral cell CP 724714 selective inhibitor

 

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