Alofanib (RPT835)

Catalog No.S8754

For research use only.

Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.

Alofanib (RPT835) Chemical Structure

CAS No. 1612888-66-0

Selleck's Alofanib (RPT835) has been cited by 1 Publication

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Biological Activity

Description Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.
Targets
FGFR2 [1]
(Cell-free assay)
In vitro

Alofanib induces mainly apoptosis with cleavage of caspase 3, PARP and Bcl-2 in SKOV3 cell line. Cytotoxic effect of compound on ovarian cancer cells is low[1]. 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 tumour 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[2].

In vivo

Intravenous alofanib significantly in dose-dependent manner potentiated the efficiency of the combination of paclitaxel and carboplatin. Alofanib suppresses angiogenesis in ovarian cancer mouse model[1]. In a FGFR-driven human tumour xenograft model, oral administration of alofanib is well tolerated and results in potent antitumour activity[2].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: SKOV3 cells
  • Concentrations: 0-1 μM
  • Incubation Time: 72 h
  • Method:

    Cells were treated with alofanib (10, 100, and 1000 μM) for 72 h and whole-cell lysates were immunoblotted.

Animal Research:

[2]

  • Animal Models: C57Bl/6 × DBA/2 F1 mice
  • Dosages: 15 mg/kg/d
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 413.40
Formula

C19H15N3O6S

CAS No. 1612888-66-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(C=C1C2=CN=CC=C2)NS(=O)(=O)C3=CC=CC(=C3)C(=O)O)[N+](=O)[O-]

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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