Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GDC-0879 (AR-00341677) is a novel, potent and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 32.00 | |
2 mg | In stock | $ 45.00 | |
5 mg | In stock | $ 72.00 | |
10 mg | In stock | $ 113.00 | |
25 mg | In stock | $ 228.00 | |
50 mg | In stock | $ 372.00 | |
100 mg | In stock | $ 597.00 | |
200 mg | In stock | $ 849.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 79.00 |
Description | GDC-0879 (AR-00341677) is a novel, potent and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well. |
Targets&IC50 | B-Raf:0.13 nM |
In vitro | GDC-0879 also inhibits cellular pERK with IC50 of 63 nM. GDC-0879 shows comparable potency in A375 melanoma and Colo205 colorectal carcinoma cell lines, both of which are B-RafV600E mutant, with IC50 of 59 nM and 29 nM for pMEK1 inhibition respectively. GDC-0879 potently inhibits B-RafV600E in Malme3M cells with IC50 of 0.75 μM. GDC-0879 also shows EC50 values < 0.5 μM in many tumor cells (A375, 624, SK-MEL-28, Malme3M, C32, 928, 888, G-361, Colo205, Colo206, SW1417, CL34, and Colo201). [1] |
In vivo | In GDC-0879 treated mice, both cell line- and patient-derived BRAFV600E tumors exhibit stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared to mutant KRAS-expressing tumors. Although there is involvement of activated RAF signaling in RAS-induced tumorigenesis, decreased time to progression is observed for some KRAS-mutant tumors following GDC-0879 administration. Whereas GDC-0879-mediated efficacy is associated strictly with B-RafV600E status, MEK inhibition also attenuates proliferation and tumor growth of cell lines expressing wild-type BRAF (81% KRAS mutant, 38% KRAS wild type). The responsiveness of B-RafV600E melanoma cells to GDC-0879 could be dramatically altered by pharmacologic and genetic modulation of PI3K pathway activity. [2] |
Synonyms | GDC 0879, AR-00341677, GDC0879 |
Molecular Weight | 334.37 |
Formula | C19H18N4O2 |
CAS No. | 905281-76-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 33.4 mg/mL (100 mM)
You can also refer to dose conversion for different animals. More
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GDC-0879 905281-76-7 MAPK Raf Inhibitor GDC 0879 Raf kinases AR00341677 AR 00341677 AR-00341677 GDC0879 inhibit inhibitor