Your shopping cart is currently empty

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 | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $32 | In Stock | In Stock | |
| 2 mg | $45 | In Stock | In Stock | |
| 5 mg | $72 | In Stock | In Stock | |
| 10 mg | $113 | In Stock | In Stock | |
| 25 mg | $228 | In Stock | In Stock | |
| 50 mg | $372 | In Stock | In Stock | |
| 100 mg | $597 | In Stock | In Stock | |
| 200 mg | $849 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $79 | In Stock | In Stock |
| 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 | GDC0879, GDC 0879, AR-00341677 |
| Molecular Weight | 334.37 |
| Formula | C19H18N4O2 |
| Cas No. | 905281-76-7 |
| Smiles | OCCn1cc(c(n1)-c1ccncc1)-c1ccc2\C(CCc2c1)=N\O |
| Relative Density. | 1.37 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 150 mg/mL (448.6 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.98 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
|---|

Copyright © 2015-2026 TargetMol Chemicals Inc. All Rights Reserved.