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Flumatinib

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

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

Flumatinib

Flumatinib

🥰Excellent
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 SizePriceAvailabilityQuantity
1 mg28 €In Stock
5 mg57 €In Stock
10 mg75 €In Stock
25 mg122 €In Stock
50 mg157 €In Stock
100 mg272 €In Stock
200 mg408 €In Stock
500 mg677 €In Stock
1 mL x 10 mM (in DMSO)75 €In Stock
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Purity:99.95%
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Product Introduction

Bioactivity
Description
Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor with potential antineoplastic activity.
Targets&IC50
PDGFRβ:307.6 nM, c-Kit:2662 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
AliasHHGV678
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
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (88.87 mM)
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

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