Ravoxertinib (GDC-0994)

Catalog No.S7554

For research use only.

Ravoxertinib (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.

Ravoxertinib (GDC-0994) Chemical Structure

CAS No. 1453848-26-4

Selleck's Ravoxertinib (GDC-0994) has been cited by 44 publications

Purity & Quality Control

Choose Selective ERK Inhibitors

Biological Activity

Description Ravoxertinib (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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 M3\xfGZ2dmO2aX;uJIF{e2G7 M4H0dWlvcGmkaYTpc44hd2ZiRWLLNkBqdiCqdX3hckBCOzd3IHPlcIx{KGijcnLvdolv\yCEUlHGJHY3ODCHIH31eIFvfCCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBxcG:|cHjvdplt[XSnZDDFVmszKGyndnXsd{whUUN3MDC9JFAvODh4IN88UU4> NIjhNpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO3OlMxPid-MkizO|Y{ODZ:L3G+
A375 MVzGeY5kfGmxbjDhd5NigQ>? MkSyTY5pcWKrdHnvckBw\iCHUluyJIlvKGi3bXHuJGE{PzViY3XscJMhcGG{Yn;ybY5oKEKUQV[gWlYxOEVibYX0ZY51KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJJBpd3OyaH;yfYxifGWmIGLTT{Bt\X[nbIOsJGlEPTBiPTCwMlE1KM7:TT6= NInFc3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO3OlMxPid-MkizO|Y{ODZ:L3G+
Assay
Methods Test Index PMID
Western blot p-MEK / MEK / p-ERK / ERK / p-p90RSK / p90RSK 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 (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 439.85
Formula

C21H18ClFN6O2

CAS No. 1453848-26-4
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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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.

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