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Ravoxertinib hydrochloride

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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

Ravoxertinib hydrochloride

🥰Excellent
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
ERK2:3.1 nM, p-RSK:12 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
Relative Density.no data available
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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In Vivo Formulation Calculator (Clear solution)

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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