543681-31-8
Chemical Structure
CP-724714 succinate
- CAS No.: 543681-31-8
- Formula:C27H27N5O3·3/2C4H6O4
- Molecular Weight:646.68
IUPAC Name: 2,3-dihydro-1H-benzo[f]chromen-1-one
SMILES: OC(CCC(O)=O)=O.COCC(NC/C=C/C1=CC(C(NC2=CC(C)=C(C=C2)OC3=CN=C(C)C=C3)=NC=N4)=C4C=C1)=O.[1.5]
Biological Activity: CP-724714 succinate is an orally active and selective HER2 tyrosine kinase inhibitor with an IC50 of 10 nM. CP-724714 succinate inhibits HER2 receptor autophosphorylation and blocks the downstream Ras-Raf-Mek-Erk signaling pathway, thereby inducing cell cycle arrest and apoptosis in tumor cells. CP-724714 succinate exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC50 of 0.91 μM). CP-724714 succinate is an inhibitor of the hepatic transport receptors OATP1B1/MDR1/BSEP, and can enter hepatocytes via active uptake and trigger the accumulation of drugs and bile acids within hepatocytes. CP-724714 succinate can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection[1][2][3].
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CP-724714 succinate | CP-724714 succinate is an orally active and selective HER2 tyrosine kinase inhibitor with an IC50 of 10 nM. CP-724714 succinate inhibits HER2 receptor autophosphorylation and blocks the downstream Ras-Raf-Mek-Erk signaling pathway, thereby inducing cell cycle arrest and apoptosis in tumor cells. CP-724714 succinate exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC50 of 0.91 μM). CP-724714 succinate is an inhibitor of the hepatic transport receptors OATP1B1/MDR1/BSEP, and can enter hepatocytes via active uptake and trigger the accumulation of drugs and bile acids within hepatocytes. CP-724714 succinate can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection. | |||||||||||||||||||||
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References
- [1]. Zhou L, et al. Identification of a receptor tyrosine kinase inhibitor CP-724714 inhibits SADS-CoV related swine diarrhea coronaviruses infection in vitro. Virologica Sinica. 2023 Oct;38(5):778-786. [Content Brief]
- [2]. Jani JP, et al. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer research. 2007 Oct 15;67(20):9887-93. [Content Brief]
- [3]. Feng B, et al. Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714. Toxicological sciences : an official journal of the Society of Toxicology. 2009 Apr;108(2):492-500. [Content Brief]
