Molecular Weight(MW): 439.85
GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
Cited by 11 Publications
4 Customer Reviews
Immunoblotting studies depicting BTK, PLCγ2, ERK1/2, and p90RSK signaling in nontransduced, vector only, BTKWT, or BTKCys481Ser (BTKC481S) MYD88-mutated WM (BCWM.1) and ABC DLBCL (TMD8) cells following treatment with vehicle control, ibrutinib, or ERK1/2 inhibitors (GDC-0994) alone or with ibrutinib for 2 hours. GAPDH was used as protein loading control.
Blood, 2018, 131(18):2047-2059. Ravoxertinib (GDC-0994) purchased from Selleck.
Pancreatic acini exposed for 1 h to 300 μM of oleic acid (OA) or linoleic acid (LA) were pre-treated for 45 min with the vehicle (DMSO) or SP600125 (50 μM), GDC-0994 (50 μM) or SB202190 (50 μM) or AG-490 (50 μM) respectively. CCL2mRNA expression was analyzed by qRT-PCR with 18S as internal standard. *p<0.05, **p<0.01 as compared with untreated acini, ♦♦p<0.01 as compared with OA- or LA-treated acini.
Biochim Biophys Acta, 2015, 1852(12):2671-7. Ravoxertinib (GDC-0994) purchased from Selleck.
Icariin promotes HaCaT cell proliferation. (A) HaCaT cells were pretreated with MK-2206, GDC-0994, or medium alone without inhibitors for 2 h. Cells were then incubated with 30 μM icariin for 24, 48 and 72 h, and cell viability was measured by CCK-8 assay. (B) Western blot analysis of Cyclin D1 and D3 protein expression levels in HaCaT cells following treatment with medium alone (control), icariin, icariin with MK-2206 or icariin with GDC-0994. Data represent mean ± standard deviation of three independent experiments. *P<0.05, **P<0.01 and ***P<0.001 vs. untreated control. CCK-8, cell counting kit-8; OD, optical density.
Biochem Biophys Res Commun, 2017, 486(4):1062-1068. Ravoxertinib (GDC-0994) purchased from Selleck.
Untreated or CCL2 pre-treated BMDMs were restimulated with IFNγ/LPS for 6 h, with additional samples treated with either vehicle control (DMSO) or the ERK1/2 inhibitor GDC-0994 (50 nM). Expression of Nos2 mRNA was analyzed via qPCR. (**) = p < 0.01 vs. Untreated.
Cell Immunol, 2017, 314:63-72. Ravoxertinib (GDC-0994) purchased from Selleck.
Purity & Quality Control
Choose Selective ERK Inhibitors
|Description||GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.|
GDC-0994 potently inhibits phospho-p90RSK in tumor cells. 
|In vivo||GDC-0994 (p.o.) results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice.  In vivo, GDC-0994 (p.o.) inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways, and subsequently prevents ERK-dependent tumor cell proliferation and survival. |
|In vitro||DMSO||87 mg/mL (197.79 mM)|
|Ethanol||87 mg/mL (197.79 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02457793||Completed||Non-Small Cell Lung Cancer Metastatic Colorectal Cancer Metastatic Non Small Cell Lung Cancer Metastatic Cancers Melanoma||Genentech Inc.||June 16 2015||Phase 1|
|NCT01875705||Completed||Solid Tumor||Genentech Inc.||June 21 2013||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Could you recommend a good tolerated solvent for orally application of this compound?
GDC-0994 can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml as a clear solution.