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Obatoclax Mesylate

产品编号 T6275 CAS 803712-79-0

别名: Obatoclax, GX15-070, 奥巴克拉甲磺酸盐

Obatoclax Mesylate (GX15-070) 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。

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Obatoclax Mesylate, CAS 803712-79-0

规格	价格/CNY	货期
1 mg	￥ 359	现货
2 mg	￥ 513	现货
5 mg	￥ 763	现货
10 mg	￥ 1,390	现货
25 mg	￥ 2,490	现货
50 mg	￥ 3,720	现货
100 mg	￥ 5,350	现货
1 mL * 10 mM (in DMSO)	￥ 717	现货

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其他形式的 Obatoclax Mesylate:

Obatoclax
询价

选择批次

纯度: 99.67%

纯度: 99.38%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Obatoclax Mesylate (GX15-070) 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.
靶点活性	BCL2:220 nM (Ki, cell free)
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].

别名	Obatoclax, GX15-070, 奥巴克拉甲磺酸盐
分子量	413.49
分子式	C20H19N3O·CH4O3S
CAS No.	803712-79-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 77 mg/mL (186.2 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4184 mL	12.0922 mL	24.1844 mL	60.461 mL
	5 mM	0.4837 mL	2.4184 mL	4.8369 mL	12.0922 mL
	10 mM	0.2418 mL	1.2092 mL	2.4184 mL	6.0461 mL
	20 mM	0.1209 mL	0.6046 mL	1.2092 mL	3.023 mL
	50 mM	0.0484 mL	0.2418 mL	0.4837 mL	1.2092 mL
	100 mM	0.0242 mL	0.1209 mL	0.2418 mL	0.6046 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Nguyen M, et al. Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7. Epub 2007 Nov 26. 2. Konopleva M, et al. Mechanisms of Antileukemic Activity of the Novel Bcl-2 Homology Domain-3 Mimetic GX15-070 (Obatoclax). Cancer Res May 1, 2008 68; 3413 3. Huang S, et al. BH3 mimetic obatoclax enhances TRAIL-mediated apoptosis in human pancreatic cancer cells. Clin Cancer Res. 2009 Jan 1;15(1):150-9. 4. Champa D, et al. Obatoclax kills anaplastic thyroid cancer cells by inducing lysosome neutralization and necrosis. Oncotarget. 2016 Jun 7;7(23):34453-71. 6. Wei WJ, et al. Obatoclax and LY3009120 Efficiently Overcome RG7204 Resistance in Differentiated Thyroid Cancer. Theranostics. 2017 Feb 23;7(4):987-1001.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Obatoclax Mesylate 803712-79-0 Apoptosis Autophagy Microbiology/Virology BCL Parasite Inhibitor broad-spectrum degradation BH3 anti-cancer mimetic Bcl-2 Family antiparasitic Obatoclax GX15-070 cancer colorectal proteasomal inhibit 奥巴克拉甲磺酸盐 human inhibitor

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Obatoclax Mesylate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords