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AST 487

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Catalog No. T4053Cas No. 630124-46-8
Alias NVP-AST 487

AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.

AST 487

AST 487

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Purity: 99.56%
Catalog No. T4053Alias NVP-AST 487Cas No. 630124-46-8
AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$31In StockIn Stock
2 mg$44In StockIn Stock
5 mg$72In StockIn Stock
10 mg$122In StockIn Stock
25 mg$197In StockIn Stock
50 mg$372In StockIn Stock
100 mg$556In StockIn Stock
500 mg$1,220-In Stock
1 mL x 10 mM (in DMSO)$84In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.56%
Color:White
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Product Introduction

AST 487 AI Summary
AST 487 demonstrates potent multi-kinase inhibitory activity, exhibiting high binding affinities (low Kd values) for several kinase domains including FLT3 (IC50: 5.012 nM), ABL1, KIT (Kd: 5.4 nM), and its D816V mutant (Kd: 360.0 nM), MET, RET, and SYK. Additionally, it inhibits NEK kinases NEK1, NEK4, NEK5, NEK6, and NEK9, with the strongest binding to NEK4. The compound shows notable inhibition of the VEGFR2 kinase domain (IC50: 3.0 nM), MEK7 (IC50: 260.0 nM), as well as MNK1 (IC50: 1760.0 nM) and MNK2 (IC50: 20.0 nM). Specific cell line assays illustrate variable impacts on cell growth rates. The diverse inhibitory effects suggest significant therapeutic potential in targeting multiple kinase-related pathways..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
Targets&IC50
FLT3:520 nM., RET:880 nM
SynonymsNVP-AST 487
Chemical Properties
Molecular Weight529.56
FormulaC26H30F3N7O2
Cas No.630124-46-8
SmilesC(C1=C(C(F)(F)F)C=C(NC(NC2=CC=C(OC=3C=C(NC)N=CN3)C=C2)=O)C=C1)N4CCN(CC)CC4
Relative Density.1.341 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 50 mg/mL (94.42 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.78 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 mM1.8884 mL9.4418 mL18.8836 mL94.4180 mL
5 mM0.3777 mL1.8884 mL3.7767 mL18.8836 mL
10 mM0.1888 mL0.9442 mL1.8884 mL9.4418 mL
20 mM0.0944 mL0.4721 mL0.9442 mL4.7209 mL
50 mM0.0378 mL0.1888 mL0.3777 mL1.8884 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:
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

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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

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