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Flumatinib

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Catalog No. T4320Cas No. 895519-90-1
Alias HHGV678

Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor with potential antineoplastic activity.

Flumatinib

Flumatinib

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Purity: 99.95%
Catalog No. T4320Alias HHGV678Cas No. 895519-90-1
Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor with potential antineoplastic activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$61In StockIn Stock
10 mg$79In StockIn Stock
25 mg$129In StockIn Stock
50 mg$166In StockIn Stock
100 mg$287In StockIn Stock
200 mg$430In StockIn Stock
500 mg$713-In Stock
1 mL x 10 mM (in DMSO)$79In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.95%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor with potential antineoplastic activity.
Targets&IC50
c-Kit:2662 nM, PDGFRβ:307.6 nM, c-ABL:1.2 nM
In vitro
In higher concentration, HH-GV-678 can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, HH-GV-678 has no or little effect on other tyrosine kinases including EGFR, KDR, c-Src and HER2. HH-GV-678 can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. Flumatinib effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820 g, N822K, Y823D, and A829P).
In vivo
The purpose of this study was to identify the metabolites of flumatinib in CML patients, with the aim of determining the main metabolic pathways of lumatinib in humans after oral administration. Ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry revealed 34 metabolites; 7 primary metabolites were confirmed by comparison with synthetic reference standards. The results show that the parent drugflumatinib was the main form recovered in human plasma, urine, and feces. The main metabolites of flumatinib in humans were the products of N-demethylation, N-oxidation, hydroxylation, and amide hydrolysis
SynonymsHHGV678
Chemical Properties
Molecular Weight562.59
FormulaC29H29F3N8O
Cas No.895519-90-1
SmilesCN1CCN(Cc2ccc(cc2C(F)(F)F)C(=O)Nc2cnc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
Relative Density.1.340 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 100 mg/mL (177.75 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.55 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 mM1.7775 mL8.8875 mL17.7749 mL88.8747 mL
5 mM0.3555 mL1.7775 mL3.5550 mL17.7749 mL
10 mM0.1777 mL0.8887 mL1.7775 mL8.8875 mL
20 mM0.0889 mL0.4444 mL0.8887 mL4.4437 mL
50 mM0.0355 mL0.1777 mL0.3555 mL1.7775 mL
100 mM0.0178 mL0.0889 mL0.1777 mL0.8887 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
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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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