货号	规格	价格	上海	北京	珠海	重庆	武汉
V48009-5mg	≥98%	￥2640.00 V48009-5mg ￥2640.00 3-5天	0 货期：3-5天	-	-	-	-
V48009-10mg	≥98%	￥4190.00 V48009-10mg ￥4190.00 3-5天	0 货期：3-5天	-	-	-	-
V48009-25mg	≥98%	￥7530.00 V48009-25mg ￥7530.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.

靶点：

Bax

体外研究：

GL0388 (0.1-10 μM; 72 h) inhibits the cell proliferation of MDA-MB-231 and MCF-7 breast cancer cell lines, with IC50s of 0.96 μM and 0.52 μM, respectively.
GL0388 (0.01-100 μM) inhibits the cell proliferation in 60 human tumor cell lines, with GI550s of 0.299-1.57 μM.
GL0388 (1-10 μM; 48 h) significantly upregulates the cleaved PARP-1 and cleaved caspase 3 in MDA-MB-231 cells.
GL0388 (0.1-1 μM; 24 h) inhibits the colony formation and invasion of breast cancer cells.
GL0388 (1-10 μM; 24 h) promotes Bax insertion into mitochondrial membranes of MDA-MB-231 cells in a dose-dependent manner. GL0388 increases cytochrome c in the cytosolic fraction of MDA-MB-231 cells.

体内研究：

GL0388 (10-20 mg/kg for i.p.; 15 mg/kg for i.t.; once daily for 10 days) dose-dependently suppresses the growth of MDA-MB-231 tumors in mice.

参考文献：

1. Liu G, et, al. Further lead optimization on Bax activators: Design, synthesis and pharmacological evaluation of 2-fluoro-fluorene derivatives for the treatment of breast cancer. Eur J Med Chem. 2021 Jul 5;219:113427.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.009 ml	15.043 ml	30.087 ml
5 mM	0.602 ml	3.009 ml	6.017 ml
10 mM	0.301 ml	1.504 ml	3.009 ml
50 mM	0.06 ml	0.301 ml	0.602 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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