1. Protein Tyrosine Kinase/RTK
  2. Bcr-Abl
    c-Kit
    PDGFR
  3. Flumatinib mesylate

Flumatinib mesylate (Synonyms: HHGV678 mesylate)

Cat. No.: HY-13905 Purity: 99.97%
Handling Instructions

Flumatinib mesylate (HH-GV-678 mesylate), a derivative of imatinib, is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit respectively.

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Flumatinib mesylate Chemical Structure

Flumatinib mesylate Chemical Structure

CAS No. : 895519-91-2

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10 mM * 1 mL in Water USD 132 In-stock
Estimated Time of Arrival: December 31
500 mg USD 120 In-stock
Estimated Time of Arrival: December 31
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Description

Flumatinib mesylate (HH-GV-678 mesylate), a derivative of imatinib, is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit respectively. IC50 Value: 1.2 nM (c-Abl); 307.6 nM(PDGFRβ); 2662 nM (c-Kit) [1] Target: c-Abl; c-Kit; PDGRFβ in vitro: HH-GV-678 can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. 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 kinase including EGFR/KDR/c-Src andHER2 [1]. Flumatinib effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820G, N822K, Y823D, and A829P) [2]. 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 offlumatinib 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 [3].

Clinical Trial
Molecular Weight

658.69

Formula

C₃₀H₃₃F₃N₈O₄S

CAS No.

895519-91-2

SMILES

O=C(NC1=CC(NC2=NC=CC(C3=CC=CN=C3)=N2)=C(C)N=C1)C4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (75.91 mM; Need ultrasonic)

DMSO : 50 mg/mL (75.91 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5182 mL 7.5908 mL 15.1816 mL
5 mM 0.3036 mL 1.5182 mL 3.0363 mL
10 mM 0.1518 mL 0.7591 mL 1.5182 mL
*Please refer to the solubility information to select the appropriate solvent.
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Keywords:

FlumatinibHHGV678HHGV 678HHGV-678Bcr-Ablc-KitPDGFRSCFRCD117Platelet-derived growth factor receptorInhibitorinhibitorinhibit

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Flumatinib mesylate
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HY-13905
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