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

Flumatinib 

Cat. No.: HY-13904 Purity: 99.83%
Data Sheet SDS Handling Instructions

Flumatinib 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.

For research use only. We do not sell to patients.
Flumatinib Chemical Structure

Flumatinib Chemical Structure

CAS No. : 895519-90-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO $87 In-stock
5 mg $70 In-stock
10 mg $90 In-stock
50 mg $190 In-stock
100 mg   Get quote  
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Other Forms of Flumatinib:

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  • Technical Information

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  • References

Description

Flumatinib 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 and HER2 [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 off 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 [3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02511340 Jiangsu Hansoh Pharmaceutical Co., Ltd. Chronic Myelogenous Leukemia January 2013 Phase 2
NCT01503502 Jiangsu HengRui Medicine Co., Ltd. Myelogenous Leukemia, Chronic August 2011 Phase 2
NCT02204644 Jiangsu Hansoh Pharmaceutical Co., Ltd. CML, CML-CP,MMR,TKI June 2014 Phase 3
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References
Molecular Weight

562.59

Formula

C₂₉H₂₉F₃N₈O

CAS No.

895519-90-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 32 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Flumatinib
Cat. No.:
HY-13904
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