Ravoxertinib (GDC-0994)

For research use only.

Catalog No.S7554

35 publications

Ravoxertinib (GDC-0994) Chemical Structure

CAS No. 1453848-26-4

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 299 In stock
USD 197 In stock
USD 497 In stock
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Selleck's Ravoxertinib (GDC-0994) has been cited by 35 publications

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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 NYXSXlZDTnWwY4Tpc44h[XO|YYm= M3e5[WlvcGmkaYTpc44hd2ZiRWLLNkBqdiCqdX3hckBCOzd3IHPlcIx{KGijcnLvdolv\yCEUlHGJHY3ODCHIH31eIFvfCCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBxcG:|cHjvdplt[XSnZDDFVmszKGyndnXsd{whUUN3MDC9JFAvODh4IN88UU4> MnzJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|N{[zNFYoRjJ6M{e2N|A3RC:jPh?=
A375 NGjuWmFHfW6ldHnvckBie3OjeR?= M{\RSmlvcGmkaYTpc44hd2ZiRWLLNkBqdiCqdX3hckBCOzd3IHPlcIx{KGijcnLvdolv\yCEUlHGJHY3ODCHIH31eIFvfCCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBxcG:|cHjvdplt[XSnZDDSV2shdGW4ZXzzMEBKSzVyIE2gNE4yPCEQvF2u NX:3UYVvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizO|Y{ODZpPkK4N|c3OzB4PD;hQi=>

... Click to View More Cell Line Experimental Data

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)
Water Insoluble
Ethanol '87 mg/mL
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
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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

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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