Angiogenesis Bcr-Abl Flumatinib


Catalog No. T4320   CAS 895519-90-1
Synonyms: HHGV678, HHGV678

Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.

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Flumatinib, CAS 895519-90-1
Pack Size Availability Price/USD Quantity
5 mg In stock 61.00
10 mg In stock 79.00
25 mg In stock 129.00
50 mg In stock 166.00
100 mg In stock 287.00
200 mg In stock 430.00
1 mL * 10 mM (in DMSO) In stock 79.00
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Purity 99.95%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.
Targets&IC50 c-Abl ,   PDGFRβ ,   c-Kit
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
Synonyms HHGV678 , HHGV678
Purity 99.95%
Molecular Weight 562.6
Formula C29H29F3N8O
CAS No. 895519-90-1


Powder: -20°C for 3 years

In solvent: -80°C for 6 months

Solubility Information

DMSO: 32 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )


References and Literature
1. Luo H, et al. HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance. Leukemia. 2010 Oct;24(10):1807-9. 2. Zhao J, et al. Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2014 Jan;105(1):117-25 3. Gong A, et al. Metabolism of flumatinib, a novel antineoplastic tyrosine kinase inhibitor, in chronic myelogenous leukemia patients. Drug Metab Dispos. 2010 Aug;38(8):1328-40.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-Cancer Compound Library Clinical Compound Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Fluorochemical Library Angiogenesis related Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Pancreatic Cancer Compound Library Cytoskeletal Signaling Pathway Compound Library Anti-Fibrosis Compound Library

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