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Flumatinib

Catalog No. T4320 CAS 895519-90-1

Synonyms: HHGV678

Flumatinib (HHGV678) 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
1 mg	In stock	$ 30.00
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
500 mg	In stock	$ 713.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.95%

Purity: 99.52%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.
Targets&IC50	c-Kit:2662 nM, PDGFRβ:307.6 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

Synonyms	HHGV678
Molecular Weight	562.59
Formula	C29H29F3N8O
CAS No.	895519-90-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (88.87 mM)

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：

Inhibitor Library FDA-Approved Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library FDA-Approved & Pharmacopeia Drug Library

Related Products

Related compounds with same targets

Imatinib impurities3 Cenisertib CHMFL-ABL-121 Imatinib Berbamine dihydrochloride CHMFL-ABL-039 PP121 DPH

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Flumatinib 895519-90-1 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl PDGFR c-Kit Inhibitor HHGV 678 HHGV-678 inhibit Platelet-derived growth factor receptor HHGV678 CD117 SCFR inhibitor

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