Ravoxertinib (GDC-0994)

Catalog No.S7554

Ravoxertinib (GDC-0994) Chemical Structure

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.

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USD 497 In stock
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Cited by 16 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

Biological Activity

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.
Targets
ERK2 [1]
(Cell-free assay)
ERK1 [1]
(Cell-free assay)
0.3 nM 1.1 nM
In vitro

GDC-0994 potently inhibits phospho-p90RSK in tumor cells. [1]

Assay
Methods Test Index PMID
Western blot
p-MEK / MEK / p-ERK / ERK / p-p90RSK / p90RSK ; 

PubMed: 28982154     


Pathway reactivation at the level of p-p90RSK was assessed in KRAS mutant cells, HCT116, using single agent cobimetinib at EC50 concentrations of 0.25 μM or GDC-0994 at 1.25 μM (HCT116 (KRASG13D, colorectal)) at indicated time points. 

28982154
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. [1] 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. [2]

Protocol

Solubility (25°C)

In vitro DMSO 87 mg/mL (197.79 mM)
Ethanol 87 mg/mL (197.79 mM)
Water Insoluble
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.
5mg/mL

* 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.

Chemical Information

Molecular Weight 439.85
Formula

C21H18ClFN6O2

CAS No. 1453848-26-4
Storage powder
in solvent
Synonyms N/A

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Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    Could you recommend a good tolerated solvent for orally application of this compound?

  • Answer:

    GDC-0994 can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml as a clear solution.

ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID