Ravoxertinib (GDC-0994)

For research use only.

Catalog No.S7554

30 publications

Ravoxertinib (GDC-0994) Chemical Structure

CAS No. 1453848-26-4

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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Selleck's Ravoxertinib (GDC-0994) has been cited by 30 publications

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
Smiles CN1C(=CC=N1)NC2=NC=CC(=N2)C3=CC(=O)N(C=C3)C(CO)C4=CC(=C(C=C4)Cl)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*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).

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02457793 Completed Drug: Cobimetinib|Drug: GDC-0994 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 Drug: GDC-0994 Solid Tumor Genentech Inc. June 21 2013 Phase 1

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

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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