GDC-0879 Inhibitor CAS No. 905281-76-7

Cat. No.	Name	Size	Price
KI0311	GDC-0879	2 mg	$193.6
	GDC-0879	5 mg	$299.2
	GDC-0879	10 mg	$475.2
	GDC-0879	25 mg	$827.2

Chemical Characteristic

Product Name	GDC-0879
CAS No.	905281-76-7
Molecular Weight	334.37
Formula	C₁₉H₁₈N₄O₂
Chemical Name	2,3-Dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-1H-inden-1-one oxime
Smiles	C(Cn1nc(c(c1)c1cc2CC/C(=N\O)/c2cc1)c1ccncc1)O
Chemical Structure

Biological activities

GDC-0879 is a highly selective and orally bioavailable RAF small-molecule inhibitor. GDC-0879 shows significant, equipotent inhibition of wild-type BRAF, BRAF^V600E, and CRAF as determined by in vitro inhibition of purified enzymes.^[1] In various vitro and cell-based assays, GDC-0879 has an IC50 of 0.13 nM against purified B-Raf V600E enzyme and a cellular pERK IC50 of 63 nM in the MALME-3M cell line. GDC-0879 has comparable in vitro potency in A375 melanoma and Colo205 colorectal carcinoma cell lines, both of which are V600E B-Raf mutant, with IC50 estimates of pMEK1 inhibition of 59 and 29 nM, respectively. ^[2] In vitro, at a final concentration of 1 µM, GDC-0879 inhibits RAF kinases by >90% and casein kinase-1δ by >50%. In vivo, in the KRAS-mutant model, GDC-0879 inhibits MEK signaling, resulting in a significant proportion of complete tumor responses. In GDC-0879-treated mice, GDC-0879 has stronger and more sustained pharmacodynamic inhibition of both cell line-and patient-derived BRAF^V600E compared with mutant KRAS-expressing tumors. ^[1] GDC-0879 inhibits the phosphorylation of MEK1 with in vivo IC50 value of 3.06 µM in plasma. ^[2]

Protocols

GDC-0879 are formulated in 0.5% methylcellulose, 0.2% Tween 80 and administered daily by oral gavage. ^[1]

References

[1] Hoeflich KP, et al. Antitumor Efficacy of the Novel RAF Inhibitor GDC-0879 Is Predicted by BRAF^V600E Mutational Status and Sustained Extracellular Signal-Regulated Kinase/ Mitogen- Activated Protein Kinase Pathway Suppression. Cancer Res. 2009, 69(7): 3042-3051. [2] Wong H, et al. Pharmacodynamics of 2-{4-[(1E)-1-(Hydroxyimino)-2, 3-dihydro-1H-inden-5- yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl}ethan-1-ol (GDC-0879), a Potent and Selective B-Raf Kinase Inhibitor: Understanding Relationships between Systemic Concentrations, Phosphorylated Mitogen-Activated Protein Kinase Kinase 1 Inhibition, and Efficacy. J Pharmacol Exp Ther. 2009, 329(1): 360-367.

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