CP-724714 Inhibitor CAS No. 537705-08-1

Cat. No.	Name	Size	Price	Add Cart
KI3460	CP-724714	5 mg	$200

Chemical Characteristic

Product Name	CP-724714
CAS No.	537705-08-1
Molecular Weight	469.53
Formula	C₂₇H₂₇N₅O₃
Chemical Name	2-Methoxy-N-[3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]acetamide
Smiles	C(=O)(COC)NC/C=C/c1cc2c(ncnc2cc1)Nc1cc(c(cc1)Oc1cnc(cc1)C)C
Chemical Structure

Biological activities

CP-724,714 is a selective inhibitor of epidermal growth factor 2(erbB/2) tyrosine kinase. In vitro tests show that CP-724,714 is against epidermal growth factor 2 tyrosine kinase with IC50 of 6.4µM. CP-724,714 also shows antiproliferative effects across a panel of human breast cancer cell lines such as BT-474 and SKBR3.^[1] CP-724,714 potently reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain with IC50 of 32 nM. CP-724,714 induces the accumulation of cells in G1 phase and a marked reduction in S phase in BT-474 cells. CP-724,714, at 1 and 3µM, respectively, leads to 80% cell death as indicated by a decrease in colony formation in BT-474 and SKBR3 cells. CP-724,714 displays a concentration-dependent inhibition of cholyl-lysyl fluorescein and taurocholate efflux into canaliculi in cryopreserved and fresh cultured human hepatocytes, respectively. CP-724,714 inhibits taurocholate transport in membrane vesicles expressing human bile salt export pump with an IC50 of 16 µM and inhibits the major efflux transporter in bile canaliculi, multidrug resistance protein 1 (MDR1), with an IC50 of ~28 µM.^[2] In vivo, CP-724,714 causes about 75% reduction of tumor erbB2 receptor phosphorylation at 30 minutes in athymic mice bearing FRE-erbB2 xenografts after the mice are administrated with CP-724,714. CP-724,714 treatments also result in a time-and dose-dependent induction of apoptosis of tumor cells in athymic mice.^[1]

Protocols

CP-724,714 is formulated in 0.5% methylcellulose in vivo and dissolved in DMSO and diluted in WEM containing 5% FBS to a final DMSO concentration of 0.4% in vitro.^[1]

References

[1] Jani JP, Finn RS, Campbell M, Coleman KG, Connell RD, Currier N, Emerson EO, Floyd E, Harriman S, Kath JC, Morris J, Moyer JD, Pustilnik LR, Rafidi K, Ralston S, Rossi AM, Steyn SJ, Wagner L, Winter SM, Bhattacharya SK. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer Res. 2007, 67(20):9887-9893. [2] Feng B, Xu JJ, Bi YA, Mireles R, Davidson R, Duignan DB, Campbell S, Kostrubsky VE, Dunn MC, Smith AR, Wang HF. 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.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com