Alofanib

SKU: orb1302071

Description

Alofanib

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1612888-66-0
• MW: 413.4
• Purity: 99.06%
• Formula: C₁₉H₁₅N₃O₆S
• SMILES: Cc1cc(c(NS(=O)(=O)c2cccc(c2)C(O)=O)cc1-c1cccnc1)[N+]([O-])=O
• Target: Apoptosis,FGFR
• Solubility: DMSO:55 mg/mL (133.04 mM);H2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.84 mM)

Bioactivity

• Target IC50:
  FGFR2:<10 nM
• In Vivo:
  Alofanib (i.v.) significantly in a dose-dependent manner potentiated the efficiency of the combination of paclitaxel and carboplatin. Alofanib suppresses angiogenesis in the ovarian cancer mouse model. In an FGFR-driven human tumor xenograft model, oral administration of alofanib is well tolerated and results in potent antitumor activity.
• In Vitro:
  In SKOV3 cell line, Alofanib induces mainly apoptosis with cleavage of caspase 3, PARP and Bcl-2. It has a low cytotoxic effect on ovarian cancer cells . Alofanib inhibits phosphorylation of FRS2α with the IC50 values of 7 and 9 nmol/l in cancer cells expressing different FGFR2 isoforms. In a panel of four cell lines representing several tumor types (triple-negative breast cancer, melanoma, and ovarian cancer), alofanib inhibits FGF-mediated proliferation with 50% growth inhibition (GI50) values of 16-370 nmol/l. Alofanib dose-dependently inhibits the proliferation and migration of human and mouse endothelial cells (GI50: 11-58 nmol/l) compared with brivanib and bevacizumab .
• Cell Research:
  SKOV3 cells were treated with alofanib (10, 100, and 1000 μM) for 72 h and whole-cell lysates were immunoblotted.

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

RPT 835, RPT835, RPT-835, Alofanib, Apoptosis, Fibroblast growth factor receptor, FGFR, FGFR2, Inhibitor, inhibit

Compound Identifiers

PubChem CID

86280646