Home Angiogenesis FGFR inhibitor Alofanib (RPT835) For research use only.

Alofanib (RPT835)

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

Alofanib (RPT835) Chemical Structure

CAS: 1612888-66-0

Selleck's Alofanib (RPT835) has been cited by 2 publications

Purity & Quality Control

Batch: S875401 DMSO] 83 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.76%
99.76

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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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models C57Bl/6 × DBA/2 F1 mice
Dosages 15 mg/kg/d
Administration i.p.

Chemical Information & Solubility

Molecular Weight 413.40 Formula

C19H15N3O6S
CAS No. 1612888-66-0 SDF --
Smiles CC1=CC(=C(C=C1C2=CN=CC=C2)NS(=O)(=O)C3=CC=CC(=C3)C(=O)O)[N+](=O)[O-]
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 83 mg/mL ( (200.77 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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