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產品描述： Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM |
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靶點：
IC50: 14 nM (Axl kinase);TAMReceptor |
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. |
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溶解性：
DMSO : 25 mg/mL (49.34 mM; ultrasonic and warming and heat to 60°C) |
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保存條件：
-20℃ |
配置溶液濃度參考：
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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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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京