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ERK-IN-3 (Alias: ASN007 free base)

Catalog No. T9141 Copy Product Info
Purity: 99.76%
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ERK-IN-3 (ASN007 free base) is a potent and orally active inhibitor of ERK. It inhibits ERK1/2 with low single-digit nM IC50 values. It can be used for the research of cancers driven by RAS mutations.

ERK-IN-3

Copy Product Info
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Catalog No. T9141
Alias ASN007 free base

ERK-IN-3 (ASN007 free base) is a potent and orally active inhibitor of ERK. It inhibits ERK1/2 with low single-digit nM IC50 values. It can be used for the research of cancers driven by RAS mutations.

ERK-IN-3
Cas No. 2055597-12-9
Pack SizePriceUSA StockGlobal StockQuantity
1 mg$56In StockIn Stock
5 mg$126In StockIn Stock
10 mg$183In StockIn Stock
25 mg$297In StockIn Stock
50 mg$486In StockIn Stock
1 mL x 10 mM (in DMSO)$127In StockIn Stock
In stock · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.76%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
ERK-IN-3 (ASN007 free base) is a potent and orally active inhibitor of ERK. It inhibits ERK1/2 with low single-digit nM IC50 values. It can be used for the research of cancers driven by RAS mutations.
In vitro
ERK-IN-3 shows single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines.ERK-IN-3 inhibits the phosphorylation of ERK1/2 substrates like RSK1, FRA1, and Elk1 in various cell lines. 
In vivo
ERK-IN-3 (daily p.o.) inhibits tumor growth in multiple BRAF and KRAS mutant xenograft models in mice that was well tolerated at efficacious doses.
SynonymsASN007 free base
Chemical Properties
Molecular Weight473.93
FormulaC22H25ClFN7O2
Cas No.2055597-12-9
SmilesCc1cnc(NC2CCOCC2)nc1-n1cnc(c1)C(=O)N[C@H](CN)c1cc(F)cc(Cl)c1
Relative Density.1.48 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 250 mg/mL (527.5 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.55 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
1mg5mg10mg50mg
1 mM2.1100 mL10.5501 mL21.1002 mL105.5008 mL
5 mM0.4220 mL2.1100 mL4.2200 mL21.1002 mL
10 mM0.2110 mL1.0550 mL2.1100 mL10.5501 mL
20 mM0.1055 mL0.5275 mL1.0550 mL5.2750 mL
50 mM0.0422 mL0.2110 mL0.4220 mL2.1100 mL
100 mM0.0211 mL0.1055 mL0.2110 mL1.0550 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

Keywords

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