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Angiogenesis Bcr-Abl Flumatinib

Flumatinib

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

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

Flumatinib, CAS 895519-90-1
Pack Size Availability Price/USD Quantity
5 mg In stock 68.00
10 mg In stock 88.00
25 mg In stock 144.00
50 mg In stock 185.00
100 mg In stock 319.00
200 mg In stock 478.00
1 mL * 10 mM (in DMSO) In stock 88.00
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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

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 32 mg/mL

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

Citations

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 Anti-cancer Clinical Compound Library

Related Products

Related compounds with same targets
Nilotinib (monohydrochloride monohydrate) Sorafenib Sorafenib tosylate A1155463 KW2449 Regorafenib monohydrate Bosutinib D8 PDGFRα kinase inhibitor 1

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Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.