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GL0388
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GL0388图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
GL0388 是一种Bax激活剂,可导致 Bax 插入线粒体膜。GL0388 对多种癌细胞具有抗增殖活性,IC50值为 0.299-1.57 μM。GL0388 激活 Bax 并诱导 Bax 介导的细胞凋亡。GL0388 在体内抑制乳腺癌异种移植肿瘤的生长。
生物活性

GL0388 is aBaxactivator that results inBaxinsertion into mitochondrial membrane. GL0388 shows antiproliferative activities against variouscancercells, withIC50s of 0.299-1.57 μM. GL0388 activatesBaxand induce Bax-mediatedapoptosis. GL0388 suppresses breastcancerxenograft tumor growth in vivo[1].

IC50& Target[1]

Bax

 

体外研究
(In Vitro)

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[1].
GL0388 (0.01-100 μM) inhibits the cell proliferation in 60 human tumor cell lines, with GI550s of 0.299-1.57 μM[1].
GL0388 (1-10 μM; 48 h) significantly upregulates the cleaved PARP-1 and cleaved caspase 3 in MDA-MB-231 cells[1].
GL0388 (0.1-1 μM; 24 h) inhibits the colony formation and invasion of breast cancer cells[1].
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[1].

Cell Proliferation Assay[1]

Cell Line:MCF-7, MDA-MB-231 cells
Concentration:0.1, 0.33, 1, 3.3, 10 μM
Incubation Time:72 hours
Result:Inhibited the growth of MCF-7, MDA-MB-231 cells, with IC50s of 0.52 μM and 0.96 μM, respectively.

Western Blot Analysis[1]

Cell Line:MDA-MB-231 cells
Concentration:1, 5, 10 μM
Incubation Time:48 hours
Result:Significantly led to the upregulation of cleaved PARP-1 and cleaved caspase 3.
体内研究
(In Vivo)

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[1].

Animal Model:Female nude mice were injected MDA-MB-231 cells[1]
Dosage:10-20 mg/kg for i.p.; 15 mg/kg for i.t.
Administration:I.p and i.t. once daily for 10 days
Result:Significantly inhibited tumor growth at a dose of 15 mg/kg every other day.
I.T. administration for 10 consecutive days, with an inhibition rate of 55%, comparable to the I.P. efficacy at the dose of daily 20 mg/kg.
分子量

332.37

Formula

C21H17FN2O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.