Cat. No. Name Size Price Add Cart
KI2349CEP-324965 mg$432
CEP-3249610 mg$592
CEP-32496200 mg$3952

Chemical Characteristic

Product NameCEP-32496
SynonymsN/A
CAS No.1188910-76-0
Molecular Weight 517.46
FormulaC24H22F3N5O5
Chemical Name1-[3-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]urea
SmilesN(C(=O)Nc1noc(c1)C(C(F)(F)F)(C)C)c1cc(ccc1)Oc1ncnc2c1cc(c(c2)OC)OC
Chemical Structure

Biological activities

CEP-32496 is a potent BRAF inhibitor. CEP-32496 inhibits mitogen-activated protein (MAP)/extracellular signal-regulated (ER) kinase (MEK) phosphorylation (pMEK) MEK (mitogen-activated protein kinase\ERK kinase) phosphorylation in human melanoma (A375) and colorectal cancer (Colo-205) cell lines with IC50s of 78 and 60 nM, respectively. CEP-32496 potently binds to the RAF family of kinases (BRAFV600E and BRAFWT) In vitro with Kd values of 36 and 14 nM, respectively. CEP-32496 inhibits cellular phosphorylation against VEGFR1 and VEGFR2 in HUVECs with IC50s ranging from 1 to 2 mM. CEP-32496 inhibits phosphorylation of LCK in lymphoma cells and KIT in carcinoma cells with IC50s of 0.8 and 1.4 mM, respectively.[1]

References

[1] James J, et al. CEP-32496: a novel orally active BRAF (V600E) inhibitor with selective cellular and in vivo antitumor activity. Mol Cancer Ther. 2012, 11(4): 930-941.

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