Flumatinib

SKU: orb1221676

Description

Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.(In Vitro):Flumatinib (HH-GV-678) can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, Flumatinib can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, Flumatinib has no or little effect on other tyrosine kinase including EGFR, KDR, c-Src and HER2 . Flumatinib (HHGV678) effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820G, N822K, Y823D, and A829P) .

Key Properties

• CAS Number: 895519-90-1
• MW: 562.6
• Purity: >98% (HPLC)
• Formula: C₂₉H₂₉F₃N₈O
• SMILES: CC1=C(C=C(C=N1)NC(=O)C2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CC=C5
• Target: cAMP
• Solubility: DMSO : ≥ 32 mg/mL; 56.88 mM

Bioactivity

• In Vitro:
  Flumatinib (HH-GV-678) can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, Flumatinib can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, Flumatinib has no or little effect on other tyrosine kinase including EGFR, KDR, c-Src and HER2. Flumatinib (HHGV678) effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i. e., D820G, N822K, Y823D, and A829P).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HHGV678

Quick Database Links

Gene Symbol

cAMP