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- 產品描述: Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM
- 靶點: IC50: 14 nM (Axl kinase)
- 體內研究: Bemcentinib (R428) (125 mg/kg, p.o.) significantly blocks MDA-MB-231-luc-D3H2LN metastases development in two independent mouse models of breast cancer dissemination, suppresses both tumor angiogenesis and vascular endothelial growth factor (VEGF)-induced corneal neovascularization in vivo. Bemcentinib (R428) (75 mg/kg/day, 25 mg/kg twice daily, p.o.) makes mice keep on a high-fat diet resulted in significantly reduced weight gain and subcutaneous and gonadal fat mass
- 參考文獻:
1. Sensi M, et al. Human cutaneous melanomas lacking MITF and melanocyte differentiation antigens express a functional Axl receptor kinase. J Invest Dermatol. 2011 Dec;131(12):2448-57. 2. Holland SJ, et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 2010 Feb 15;70(4):1544-54. 3. Lijnen HR, et al. Growth arrest-specific protein 6 receptor antagonism impairs adipocyte differentiation and adipose tissue development in mice. J Pharmacol Exp Ther. 2011 May;337(2):457-64.
- 溶解度: DMSO : 25 mg/mL (49.34 mM; ultrasonic and warming and heat to 60°C)
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.974 ml 9.869 ml 19.738 ml 5 mM 0.395 ml 1.974 ml 3.948 ml 10 mM 0.197 ml 0.987 ml 1.974 ml 50 mM 0.039 ml 0.197 ml 0.395 ml
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