Flumatinib

SKU: orb1302954

Description

Flumatinib (HHGV678) is an orally administered small molecule tyrosine kinase inhibitor with potential antineoplastic properties. It is used in research for targeting BCR-ABL in chronic myeloid leukemia, demonstrating activity in both in vitro cellular assays and in vivo animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 895519-90-1
• MW: 562.59
• Purity: 99.95%
• Formula: C₂₉H₂₉F₃N₈O
• SMILES: CN1CCN(Cc2ccc(cc2C(F)(F)F)C(=O)Nc2cnc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
• Target: PDGFR,c-Kit,Bcr-Abl
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.55 mM);DMSO:50 mg/mL (88.87 mM)

Bioactivity

• Target IC50:
  PDGFRβ:307.6 nM|c-Kit:2662 nM|c-ABL:1.2 nM
• 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
• 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).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

c-Kit, cKit, CD117, Bcr-Abl, BcrAbl, c-Abl, Inhibitor, inhibit, PDGFR, PDGFRβ, Platelet-derived growth factor receptor, HHGV 678, HHGV678, HHGV-678, Flumatinib, SCFR

Compound Identifiers

PubChem CID

46848036