GL0388|西域试剂

GL0388,98.01%

产品编号：Bellancom-132173| 分子式：C₂₁H₁₇FN₂O| 分子量：332.37

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货号	价格	库存与货期
Bellancom-132173	￥2650.00	杭州北京（现货）
Bellancom-132173	￥4200.00	杭州北京（现货）
Bellancom-132173	￥8600.00	杭州北京（现货）
Bellancom-132173	￥14200.00	杭州北京（现货）

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GL0388

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 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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nude mice were injected MDA-MB-231 cells
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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nude mice were injected MDA-MB-231 cells
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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nude mice were injected MDA-MB-231 cells
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.