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Ravoxertinib (GDC-0994) ERK inhibitor

Name: Ravoxertinib (GDC-0994)
Brand: Selleck Chemicals
SKU: S7554
Availability: InStock
Rating: 5 (72 reviews)

Cat.No.S7554

Ravoxertinib (GDC-0994) is a potent, orally available and highly selective ERK1/2 inhibitor, with IC50 values of 1.1 nM and 0.3 nM, respectively. This compound is currently in Phase 1.

Chemical Structure

Molecular Weight: 439.85

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.73%

99.73

Related Targets	Ras p38 MAPK Raf JNK MEK S6 Kinase MAP4K TAK1 Mixed Lineage Kinase ASK MNK MAPKAPK2 KLF TOPK
Related Products	SCH772984 Ulixertinib (BVD-523) Temuterkib (LY3214996) FR 180204 XMD8-92 VX-11e AZD0364 (ATG-017) ERK5-IN-1 MK-8353 (SCH900353) DEL-22379 Astragaloside IV KO-947 Magnolin Senkyunolide I Pluripotin (SC1) DMU-212 CC-90003 BAY-885 AG-126

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	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

Chemical Information, Storage & Stability

Molecular Weight	439.85	Formula	C₂₁H₁₈ClFN₆O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1453848-26-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	ERK2 ^[1] (Cell-free assay) 0.3 nM ERK1 ^[1] (Cell-free assay) 1.1 nM
In vitro	Ravoxertinib (GDC-0994) potently inhibits phospho-p90RSK in tumor cells. ^[1]
In vivo	Ravoxertinib (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, this compound inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways, and subsequently prevents ERK-dependent tumor cell proliferation and survival. ^[2]
References	http://www.abstractsonline.com/Plan/ViewAbstract.aspx?mID=3404&sKey=1eb84585-6831-405d-88b2-cef74aaf004e&cKey=22cc177f-4718-4f12-bdf6-a275db718f29&mKey=6ffe1446-a164-476a-92e7-c26446874d93 https://pubmed.ncbi.nlm.nih.gov/27227380/ https://pubmed.ncbi.nlm.nih.gov/35764642/ https://pubmed.ncbi.nlm.nih.gov/36073544/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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

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

Frequently Asked Questions

Question 1:
Could you recommend a good tolerated solvent for orally application of this compound?

Answer:
It 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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