Home MAPK ERK inhibitor Ravoxertinib (GDC-0994) For research use only.

Ravoxertinib (GDC-0994)

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

Ravoxertinib (GDC-0994) Chemical Structure

CAS No. 1453848-26-4

Purity & Quality Control

Ravoxertinib (GDC-0994) Related Products

Signaling Pathway

ERK Signaling Pathways

ERK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 Function assay Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated ERK2 levels, IC50 = 0.086 μM. 28376306
A375 Function assay Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated RSK levels, IC50 = 0.14 μM. 28376306
Click to View More Cell Line Experimental Data

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
In vitro

GDC-0994 potently inhibits phospho-p90RSK in tumor cells. [1]
In Vivo
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]
Animal Research Animal Models Mice
Dosages 40 µg
Administration p.o.
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

Chemical Information & Solubility

Molecular Weight 439.85 Formula

C21H18ClFN6O2
CAS No. 1453848-26-4 SDF Download Ravoxertinib (GDC-0994) SDF
Smiles CN1C(=CC=N1)NC2=NC=CC(=N2)C3=CC(=O)N(C=C3)C(CO)C4=CC(=C(C=C4)Cl)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (200.06 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 88 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

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.

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