CEP-32496 (free base) Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling. Mutations of B-Raf, particularly at Val
600, are common in melanomas and melanocytic nevi. CEP-32496 is a potent inhibitor of B-Raf
V600E (K
d = 14 nM in an
in vitro binding assay). It blocks B-Raf
V600E-dependent phosphorylation of MEK in human melanoma A375 and colorectal cancer COLO 205 cells (IC
50s = 78 and 60 nM, respectively). CEP-32496 binds kinases other than B-Raf but displays selective cytotoxicity for cells expressing B-Raf
V600E. It displays good oral bioavailability in rats, dogs, and monkeys and has single oral dose pharmacodynamics inhibition of both pMEK and pERK in B-Raf
V600E colon carcinoma xenografts in nude mice.
Verwenden
CEP 32496 is an orally active BRAFV600E inhibitor with selective cellular and in vivo antitumor activity.
CEP-32496 (free base) Upstream-Materialien And Downstream Produkte
Upstream-Materialien
[5-(2,2,2-TRIFLUORO-1,1-DIMETHYL-ETHYL)-ISOXAZOL-3-YL]-CARBAMIC ACID PHENYL ESTER
5-(1,1,1-Trifluoro-2-methylpropan-2-yl)isoxazol-3-amine
methyl 3,3,3-trifluoro-2,2-dimethylpropanoate
1188911-73-0
3,3,3-Trifluoro-2,2-dimethylpropionic acid
3-[(6,7-dimethoxy-4-quinazolinyl)oxy]aniline
4-Chloro-6,7-dimethoxyquinazoline
3-Aminophenol
Downstream Produkte