Alofanib (RPT835) is a novel, selective FGFR2 allosteric inhibitor with a significant inhibitory effect on FGf2-induced FRS2α phosphorylation in KATO III cells with IC50 less than 10 nM. In cells, it has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels, and no effect on FGF2-FGFR2 binding.

 

Brand: BCM

 

Target: Apoptosis; FGFR

 

Signaling Pathways: Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors

 

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.

 

Boiling Point: 659.6±65.0 °C(Predicted)

 

pKa: 3.59±0.10(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: CC1=CC(=C(C=C1C2=CN=CC=C2)NS(=O)(=O)C3=CC=CC(=C3)C(=O)O)[N+](=O)[O-]  

 

InChIKey: QUQGQIASFYWKAB-UHFFFAOYSA-N  

 

InChI: InChI=1S/C19H15N3O6S/c1-12-8-18(22(25)26)17(10-16(12)14-5-3-7-20-11-14)21-29(27,28)15-6-2-4-13(9-15)19(23)24/h2-11,21H,1H3,(H,23,24)

 

Attribute
[CAS No.]	1612888-66-0
[Formula]	C19H15N3O6S
[Molecular]	413.40
[Chem Name]	3-[(4-methyl-2-nitro-5-pyridin-3-ylphenyl)sulfamoyl]benzoic acid
[Synonym]	Alofanib; RPT835
[Storage]	Inert atmosphere. Room Temperature
[MDL No.]	MFCD30533418
[Form]	A crystalline solid

Goods Tag