Alofanib (RPT835)

An allosteric inhibitor of FGFR2

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库存: 现货

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5mg

￥987.00

790.00

- +
10mg

￥1412.00

1130.00

- +
25mg

￥2825.00

2260.00

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50mg

￥4200.00

3360.00

- +
100mg

￥6475.00

5180.00

- +

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Background

Alofanib is an allosteric inhibitor of FGFR2.^1,2 It inhibits FGF2-induced phosphorylation of FGFR substrate 2 (FRS2α) in KATO III gastric carcinoma cells (IC₅₀ = <10 nM).² Alofanib inhibits the growth of SKOV3 ovarian and Hs 578T breast cancer cells (GI₅₀s = 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.¹ 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 FGFR2²

1.Khochenkov, D.A., Solomko, E.S., Peretolchina, N.M., et al.Antiangiogenic activity of alofanib, an allosteric inhibitor of fibroblast growth factor receptor 2Bull. Exp. Biol. Med.160(1)84-87(2015) 2.Tsimafeyeu, I., Ludes-Meyers, J., Stepanova, E., et al.Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour modelsEur. J. Cancer6120-28(2016)