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Enzymes for Research, Diagnostic and Industrial Use

GDC-0879

Cat No.
CEI-0156
Description
GDC-0879 can inhibit raf with IC50 of 63 nM
CAS No.
905281-76-7
Molecular Weight
334.37
Purity
>99%
Storage
2 years at -20 centigrade
Targets
raf
Molecular Formula
C19H18N4O2
Chemical Name
(E)-5-(1-(2-hydroxyethyl)-3-(pyridin-4-yl)-1H-pyrazol-4-yl)-2,3-dihydroinden-1-one oxime
Solubility
DSMO 67 mg/mL Water
In vitro
As an ATP-competitive RAF kinase inhibitor, GDC-0879 show significant, equipotent inhibition of wild-type BRAF, BRAF(V600E), and CRAF. GDC-0879 inhibit BRAF-mutant Malme3M cells with EC 50 of 0.75 uM. Tumor cells with oncogenic mutations in either KRAS or NRAS showed limited dependence on BRAF activity and were frequently resistant to GDC-0879 treatment in vitro (EC 50 > 7.5 A mol/L for 28 of 32 cell lines). Cells with GDC-0879 EC 50 values
In vivo
Following tumor establishment (200-250 mm), animals were dosed once daily with 100 mg/kg GDC-0879 by oral gavage and tumor growth was monitored by caliper measurement. Daily treatment for 21 consecutive days induced significant tumor responses in LOX-IMVI, A375, and Colo205 xenografts (93%, 85%, and 53% tumor inhibition, respectively). Rapid tumor regression was observed for the majority of LOX-IMVI tumor-bearing mice and complete responses (regression of the established tumor beyond the level of detection by palpation) or partial responses (shrinkage of at least 50% relative to starting tumor volume) were observed in 10% and 70% of the animals.
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