Obatoclax Mesylate - CAS:803712-79-0

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Obatoclax Mesylate (Synonyms:GX15-070 Mesylate)

目录号 : KM5414 CAS No. : 803712-79-0 纯度 : 98%

Data Sheet 产品使用指南

Obatoclax Mesylate (GX15-070 Mesylate) 是 BH3 模拟物，是泛 BCL-2 家族蛋白抑制剂，对 BCL-2 的 K_i 值为 220 nM。Obatoclax Mesylate 诱导自噬 (autophagy) 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。Obatoclax Mesylate 具有抗癌和广谱抗寄生虫 (antiparasitic) 活性。

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生物活性

Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a K_i of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.

体外研究

Obatoclax Mesylate (GX15-070 Mesylate) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM.
Obatoclax Mesylate (50-200 nM; 24-72 hours) induces a dose- and time-dependent reduction of cell numbers in all human colorectal cancer cell lines. In particular, the IC₅₀ of cell proliferation at 72 h are 25.85, 40.69, and 40.01 nM for HCT116, HT-29, and LoVo cells, respectively.
Obatoclax Mesylate (400 nM; for 24 hours) induces autophagy in OSCC cells.
Obatoclax Mesylate (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations.
Obatoclax Mesylate (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM.
Obatoclax Mesylate induces T286 phosphorylation-dependent or -independent cyclin D1 degradation. in HCT116 and LoVo cells, the steady-state levels of p-Cyclin D (T286) began to decline once exposed to obatoclax Mesylate (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax Mesylate inhibits GSK3β but activates p38MAPK, while barely affecting ERK1/2 activity in HT-29 cells.
Obatoclax Mesylate (50, 100, 150, 200, 250, 300, 350, 400, 450 nM) potently inhibits the clonogenic potential of oral cancer cells.

Cell Proliferation Assay

Cell Line:	human colorectal cancer HCT116, HT-29 and LoVo cells
Concentration:	50, 100, 200 nM
Incubation Time:	24, 48, and 72 hours
Result:	Induced a dose- and time-dependent reduction of cell numbers.

Cell Autophagy Assay

Cell Line:	AW8507 and SCC029B cells
Concentration:	400 nM
Incubation Time:	24 hours
Result:	Induced autophagy in OSCC cells.

Cell Cycle Analysis

Cell Line:	HCT116 and HT-29 cells
Concentration:	50, 100, 200 nM
Incubation Time:	24 hours
Result:	Provoked a dose-dependent increase in the G1-phase cell populations.

Western Blot Analysis

Cell Line:	HCT116, HT-29 and LoVo cells
Concentration:	25, 50, 100, 200 nM
Incubation Time:	24 hours
Result:	Indicated a marked drop in cyclin D1 levels as low as 50 nM.

体内研究

Obatoclax Mesylate (GX15-070 Mesylate; 1.15-5 mg/kg; intravenously injected; five consecutive days) exhibits potent antitumor activity in xenograft mouse models in a dose-dependent manner.

Animal Model:	6-8 weeks old female BALB/C nude mice bearing subcutaneous tumors
Dosage:	1.15, 2.5, 5 mg/kg
Administration:	Intravenously injected (through lateral tail vein); five consecutive days (i.e. 5 injections)
Result:	Exhibited potent antitumor activity in xenograft mouse models in a dose-dependent manner.

分子式

C₂₁H₂₃N₃O₄S

分子量

413.49

CAS号

803712-79-0

中文名称

奥巴克拉甲磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (30.23 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4184 mL	12.0922 mL	24.1844 mL
5 mM	0.4837 mL	2.4184 mL	4.8369 mL
10 mM	0.2418 mL	1.2092 mL	2.4184 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.83 mg/mL (2.01 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (2.01 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.83 mg/mL (2.01 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (2.01 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

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分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

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浓度

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KKL 顾客使用本产品发表的 7 篇科研文献

The molarity calculator equation

The dilution calculator equation