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Ravoxertinib hydrochloride

Name: Ravoxertinib hydrochloride
Brand: TargetMol
SKU: T15377
Rating: 4.5 (1 reviews)

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Catalog No. T15377Cas No. 2070009-58-2

Alias GDC-0994 (hydrochloride)

Ravoxertinib hydrochloride is an orally bioavailable and selective inhibitor for ERK kinase activity (IC50: 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively).

Ravoxertinib hydrochloride

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Catalog No. T15377Alias GDC-0994 (hydrochloride)Cas No. 2070009-58-2

Ravoxertinib hydrochloride is an orally bioavailable and selective inhibitor for ERK kinase activity (IC50: 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively).

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Product Introduction

Bioactivity

Description	Ravoxertinib hydrochloride is an orally bioavailable and selective inhibitor for ERK kinase activity (IC50: 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively).
Targets&IC50	ERK1:6.1 nM, ERK2:3.1 nM, p-RSK:12 nM
In vitro	Ravoxertinib inhibits p90RSK (IC50: 12 nM) [1]. Ravoxertinib is highly selective for ERK1 and ERK2 (biochemical potency: 1.1 nM and 0.3 nM, respectively) [2].
In vivo	Ravoxertinib (10 mg/kg; p.o.; in CD-1 mice) is sufficient to achieve the desired target coverage for at least 8 h [1]. Ravoxertinib (p.o.; daily) causes significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice [2].
Synonyms	GDC-0994 (hydrochloride)

Chemical Properties

Molecular Weight	477.32
Formula	C₂₁H₁₉Cl₂FN₆O₂
Cas No.	2070009-58-2
Smiles	Cl.Cn1nccc1Nc1nccc(n1)-c1ccn([C@H](CO)c2ccc(Cl)c(F)c2)c(=O)c1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (209.5 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.91 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0950 mL	10.4752 mL	20.9503 mL	104.7515 mL
5 mM	0.4190 mL	2.0950 mL	4.1901 mL	20.9503 mL
10 mM	0.2095 mL	1.0475 mL	2.0950 mL	10.4752 mL
20 mM	0.1048 mL	0.5238 mL	1.0475 mL	5.2376 mL
50 mM	0.0419 mL	0.2095 mL	0.4190 mL	2.0950 mL
100 mM	0.0210 mL	0.1048 mL	0.2095 mL	1.0475 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc