A selective inhibitor of HER2/ErbB2 (IC50 = 10 nM); inhibits the proliferation of ErbB2-amplified cells

CP 724,714 – 25 mg

Brand:
Cayman
CAS:
383432-38-0
Storage:
-20
UN-No:
Non-Hazardous - /

CP 724,714 is a selective inhibitor of HER2/ErbB2 with an IC50 value of 10 nM.{31036} It demonstrates greater than 640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, and c-Met.{31036} 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.{31036} It also demonstrates antitumor activity in various human tumor xenograft models.{31036} 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.{31035}  

 

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Description

A selective inhibitor of HER2/ErbB2 (IC50 = 10 nM); inhibits the proliferation of ErbB2-amplified cells, including BT474 and SK-BR-3 (IC50s = 0.25 and 0.95 μM, respectively) and demonstrates antitumor activity in various human tumor xenograft models

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

Synonyms: 

Molecular weight: 469.5

CAS: 383432-38-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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