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  3. Obatoclax Mesylate

Obatoclax Mesylate  (Synonyms: 奥巴克拉甲磺酸盐 ; GX15-070 Mesylate)

目录号: HY-10969 纯度: 99.74%
COA 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-2Ki 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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Obatoclax Mesylate Chemical Structure

Obatoclax Mesylate Chemical Structure

CAS No. : 803712-79-0

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Top Publications Citing Use of Products

    Obatoclax Mesylate purchased from MCE. Usage Cited in: Biomed Pharmacother. 2020 Sep;129:110371.  [Abstract]

    Bcl-2 and Bcl-xl protein expression levels are restrained in A549 and H1975 cells treated with RBCm-OM/PLGA; however, Bax, cleaved Caspase-3, Caspase-9 and PARP are up-regulated following RBCm-OM/PLGA incubation. Also, free Obatoclax Mesylate (OM) does not influence the expression change of all these proteins.

    Obatoclax Mesylate purchased from MCE. Usage Cited in: Biomed Pharmacother. 2020 Sep;129:110371.  [Abstract]

    Immunofluorescence staining displays weaker Bcl-2 fluorescence intensity in lung cancer cells incubated with RBCm-Obatoclax Mesylate (OM)/PLGA, accompanied with stronger expression of pro-apoptotic signal Bax in comparison to the Con group.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2[1][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[3][4].

    IC50 & Target[5]

    Bcl-2

    220 nM (Ki)

    Mcl-1

    1-7 μM (Ki)

    Bcl-xL

    1-7 μM (Ki)

    Bcl-W

    1-7 μM (Ki)

    Bcl-B

    1-7 μM (Ki)

    体外研究
    (In Vitro)

    Obatoclax Mesylate (GX15-070 Mesylate) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM[2].
    ? 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[1].
    ? Obatoclax Mesylate (400 nM; for 24 hours) induces autophagy in OSCC cells[3].
    ? Obatoclax Mesylate (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations[1].
    ? Obatoclax Mesylate (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM[1].
    ? 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[1].
    ? Obatoclax Mesylate (50-450 nM) potently inhibits the clonogenic potential of oral cancer cells[1].

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

    Cell Proliferation Assay[1]

    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[3]

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

    Cell Cycle Analysis[1]

    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[1]

    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
    (In Vivo)

    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[4].

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

    Animal Model: 6-8 weeks old female BALB/C nude mice bearing subcutaneous tumors[4]
    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.
    Clinical Trial
    分子量

    413.49

    Formula

    C21H23N3O4S

    CAS 号
    性状

    固体

    颜色

    Purple to black

    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, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 12.5 mg/mL (30.23 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    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
    查看完整储备液配制表

    * 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 (sealed storage, away from moisture and 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。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    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

    • 方案 一

      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); 澄清溶液

      此方案可获得 ≥ 0.83 mg/mL(饱和度未知)的澄清溶液。

      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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      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); 澄清溶液

      此方案可获得 ≥ 0.83 mg/mL(饱和度未知)的澄清溶液。

      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。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.74%

    参考文献

    完整储备液配制表

    * 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 (sealed storage, away from moisture and 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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4184 mL 12.0922 mL 24.1844 mL 60.4610 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
    15 mM 0.1612 mL 0.8061 mL 1.6123 mL 4.0307 mL
    20 mM 0.1209 mL 0.6046 mL 1.2092 mL 3.0230 mL
    25 mM 0.0967 mL 0.4837 mL 0.9674 mL 2.4184 mL
    30 mM 0.0806 mL 0.4031 mL 0.8061 mL 2.0154 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    目录号:
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