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Obatoclax Mesylate
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。
Obatoclax Mesylate图片
CAS NO:803712-79-0
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
奥巴克拉盐酸盐
Obatoclax
GX15-070
产品介绍
Obatoclax Mesylate 是泛BCL-2家族蛋白抑制剂,对 BCL-2 的Ki值为 220 nM。它是 BH3 模拟物,具有抗癌和广谱抗寄生虫活性。它诱导自噬依赖性细胞死亡,并靶向细胞周期蛋白 D1 进行蛋白酶体降解。

产品描述

Obatoclax is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3.

体外活性

Obatoclax (GX15-070) potently interfered with the direct interaction between MCL-1 and BAK in intact mitochondrial outer membrane and inhibited the association between MCL-1 and BAK in intact cells [1]. Obatoclax inhibited cell growth of HL-60, U937, OCI-AML3, and KG-1 cell lines. Obatoclax induced apoptosis in AML CD34+ progenitor cells with an average IC50 of 3.59 micromol/L although clonogenicity was inhibited at concentrations of 75 to 100 nmol/L [2]. Obatoclax reduced the viability of PANC-1 and BxPC-3 cell lines and synergistically enhanced TRAIL-mediated cytotoxicity [3].

体内活性

When formulated for i.v. administration, obatoclax (2 or 3.5 mg/kg) was found to have single-agent antitumor effects in several standard mouse tumor models. Antitumor activity without animal weight loss was observed in mice bearing solid tumors [1]. Thyroid cancer-carrying [Pten,Trp53]thyr?/? mice were treated with vehicle or Obatoclax for 6 days. Live thyrocytes in Obatoclax-treated mice exhibited a dramatic reduction in Lysotracker staining [4].

细胞实验

Cells were plated in logarithmic growth phase at 2,000-4,000 cells per well in 96-well clear bottom plates and cultured for 14 to 16 h before the start of drug treatment. Serial dilutions of obatoclax or companion drug were made in DMSO, diluted 1:50 in RPMI, and then added to tissue culture media at a final concentration of 0.2% DMSO. Cells were typically treated with a dose range of compound from 50 nM to 10 mM for 72 h. Cell viability was then determined using the ViaLight kit, according to the manufacturer's instructions. To obtain percentage viability, samples are expressed as a percentage of the signal obtained from DMSO-treated cells. Dose-response points were then plotted on a log scale, and IC50 values were determined using a best-fit sigmoidal dose-response curve with variable slope. The top of the curve was set to 100% [1].

动物实验

Cells were transplanted s.c. into the flank of female BALB/c or CB17 SCID/SCID mice (6 to 8 weeks of age) as a suspension in PBS (1.0×10^6 cells/ml, 1.5×10^6 cells/ml, 2.0×10^6 cells/ml, or 5.0×10^6 cells/ml for SW480, C33A, PC3, and 4T1 cells respectively. After 7 (SW480), 14 (C33A), or 8 (PC3 and 4T1) days, treatment with drug was initiated, and body weight and tumor size were measured three times per week. The mean relative tumor size and volume (cohort of eight animals per treatment) were calculated as follows: length (mm) ′ [width (mm)]2/2. Formulated obatoclax (tartrate salt) was administered intravenously (tail vein) once a day ′5 and cisplatin once every 3 days ′ 5 by the i.p. route. Obatoclax was formulated at the indicated concentration in 9.6% polyethylene glycol 300, 0.4% polysorbate 20, and 5% dextrose, except for the 4T1 tumor model where it was formulated at a concentration of 0.6 mg/ml in 9.48% polyethylene glycol, 0.38% polysorbate 20, 1.2 mg/ml mannitol, and 5% dextrose [1].

Cas No.

803712-79-0

分子式

C21H23N3O4S

分子量

413.49

别名

奥巴克拉盐酸盐;Obatoclax;GX15-070

储存和溶解度

DMSO:77 mg/mL (186.2 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years