| Name | Flumatinib |
| Description | Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor with potential antineoplastic activity. |
| 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 |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.55 mM), Sonication is recommended.
DMSO : 100 mg/mL (177.75 mM), Sonication is recommended.
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| Keywords | SCFR | Platelet-derived growth factor receptor | PDGFRβ | PDGFR | Inhibitor | inhibit | HHGV-678 | HHGV 678 | Flumatinib | c-Kit | cKit | CD117 | c-Abl | Bcr-Abl | BcrAbl |
| Inhibitors Related | Gilteritinib | Regorafenib monohydrate | Sunitinib | Toceranib Phosphate | Sorafenib | Dasatinib | Pexidartinib | Nintedanib esylate | Regorafenib | Lenvatinib mesylate | Lenvatinib | Pazopanib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
