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Ravoxertinib hydrochloride

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

Ravoxertinib hydrochloride

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
p-RSK:12 nM, ERK2:3.1 nM, ERK1:6.1 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].
AliasGDC-0994 (hydrochloride)
Chemical Properties
Molecular Weight477.32
FormulaC21H19Cl2FN6O2
Cas No.2070009-58-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (209.50 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0950 mL10.4752 mL20.9503 mL104.7515 mL
5 mM0.4190 mL2.0950 mL4.1901 mL20.9503 mL
10 mM0.2095 mL1.0475 mL2.0950 mL10.4752 mL
20 mM0.1048 mL0.5238 mL1.0475 mL5.2376 mL
50 mM0.0419 mL0.2095 mL0.4190 mL2.0950 mL
100 mM0.0210 mL0.1048 mL0.2095 mL1.0475 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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