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GDC-0879

Chemical Structure : GDC-0879

CAS No.: 905281-76-7

GDC-0879 (GDC0879;GDC 0879)

Catalog No.: PC-45877Not For Human Use, Lab Use Only.

A potent and selective B-Raf kinase inhibitor with IC50 of 0.13 nM against purified B-Raf V600E and a cellular pERK IC50 of 63 nM in the MALME-3M cell line.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GDC-0879 is a potent and selective B-Raf kinase inhibitor with IC50 of 0.13 nM against purified B-Raf V600E and a cellular pERK IC50 of 63 nM in the MALME-3M cell line.
GDC-0879 shows expected activity only against C-Raf against a panel of 140 kinases at 1 uM.
GDC-0879 shows comparable potency in A375 melanoma and Colo205 colorectal carcinoma cell lines with IC50 of 59 nM and 29 nM for pMEK1 inhibition respectively.
GDC-0879 shows tumor growth inhibition in A375 xenografts; orally active.

Physicochemical Properties

M.Wt 334.3718
Formula C19H18N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Inden-1-one, 2,3-dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-, oxime

References

1. Wong H, et al. J Pharmacol Exp Ther. 2009 Apr;329(1):360-7.

2. Hoeflich KP, et al. Cancer Res. 2009 Apr 1;69(7):3042-51.

3. Hansen JD, et al. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5.

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