An allosteric inhibitor of FGFR2; inhibits FGF2-induced phosphorylation of FRS2α in KATO III cells (IC50 = 10 nM); inhibits the growth of SKOV3 and Hs 578T cells (GI50s = 370 and 210 nM

Alofanib – 25 mg

Brand:
Cayman
CAS:
1612888-66-0
Storage:
-20
UN-No:
Non-Hazardous - /

Alofanib is an allosteric inhibitor of FGFR2.{58160,58161} It inhibits FGF2-induced phosphorylation of FGFR substrate 2 (FRS2α) in KATO III gastric carcinoma cells (IC50 = 50s = 370 and 210 nM, respectively). It inhibits proliferation of human umbilical vein endothelial cells (HUVECs) induced by basic FGF (bFGF; IC50 = 11 nM) and tube formation of SVEC4-10 endothelial cells when used at a concentration of 50 nM.{58160} It also inhibits migration of SVEC4-10 cells in a wound healing assay. Alofanib (50 mg/kg) decreases the number of microvessels in tumor tissue by 50% in a SKOV3 ovarian serous carcinoma mouse model. It reduces tumor growth in mouse xenograft models when administered at a dose of 30 mg/kg per day, and the degree of tumor volume reduction positively correlates with the expression level of FGFR2{58161}  

 

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SKU: 31754 - 25 mg Category:

Description

An allosteric inhibitor of FGFR2; inhibits FGF2-induced phosphorylation of FRS2α in KATO III cells (IC50 = 10 nM); inhibits the growth of SKOV3 and Hs 578T cells (GI50s = 370 and 210 nM, respectively); inhibits bFGF-induced HUVEC proliferation (IC50 = 11 nM); inhibits SVEC4-10 cell tube formation at 50 nM; decreases the number of tumor microvessels by 50% in a SKOV3 ovarian serous carcinoma mouse model; reduces tumor growth in mouse xenograft models at 30 mg/kg per day

Formal name: 3-[[[4-methyl-2-nitro-5-(3-pyridinyl)phenyl]amino]sulfonyl]-benzoic acid

Synonyms:  RPT835

Molecular weight: 413.4

CAS: 1612888-66-0

Purity: ≥98%

Formulation: A crystalline solid

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