Obatoclax (GX15-070) 的 Ki 值约为 1-7 μM，可抑制 BCL-2、BCL-XL、MCL-1、BCL-w、A1 和 BCL-b [2]。在所有人类结直肠癌细胞系中，obatoclax（50-200 nM；24-72 小时）会导致细胞数量呈剂量和时间依赖性减少。具体而言，72小时时，HCT116、HT-29和LoVo细胞的细胞增殖IC50值分别为25.85、40.69和40.01 nM [1]。 obatoclax (400 nM) 会在 24 小时内刺激 OSCC 细胞的自噬 [3]。 obatoclax (50-200 nM) 在 24 小时内引起 G1 细胞群的剂量依赖性增加 [1]。 obatoclax（25-200 nM；持续 24 小时）显着降低细胞周期蛋白 D1 水平；观察到的最低水平为 50 nM [1]。 Obatoclax 导致细胞周期蛋白 D1 降解，这种降解要么独立于 T286 磷酸化，要么依赖于 T286 磷酸化。暴露于 obatoclax（200 nM；1、3、6、12、24 小时）后，HCT116 和 LoVo 细胞中 p-Cyclin D (T286) 的稳态水平开始下降。在 HT-29 细胞中，obatoclax 几乎不影响 ERK1/2 活性，但会抑制 GSK3β 并激活 p38 MAPK [1]。 obatoclax (50, 100, 150, 200, 250, 300, 350, 400, 450 nM) 成功抑制口腔癌细胞的克隆形成潜力[1]。

在异种移植小鼠模型中，obatoclax（GX15-070；1.15-5 mg/kg；静脉注射；连续五天）以剂量依赖性方式表现出强大的抗癌功效[4]。

细胞增殖测定[1]
细胞类型：人类结直肠癌 HCT116、HT-29 和 LoVo 细胞
测试浓度： 50、100、200 nM
孵育持续时间：24、48 和 72 小时
实验结果：诱导剂量和时间依赖性细胞增殖减少细胞。

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自噬测定 [3]
细胞类型： AW8507 和 SCC029B 细胞
测试浓度： 400 nM
孵育持续时间：24小时
实验结果：在OSCC细胞中诱导自噬。

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细胞周期分析[1]
细胞类型： HCT116 和 HT-29 细胞
测试浓度： 50、100、200 nM
孵育持续时间：24小时
实验结果：引起G1期细胞群的剂量依赖性增加。

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蛋白质印迹分析[1]
细胞类型： HCT116、HT-29 和 LoVo 细胞
测试浓度： 50、100、 200 nM
孵育持续时间：24 小时
实验结果：证明细胞周期蛋白 D1 水平显着降低，低至 50 nM。

Animal/Disease Models: 6-8 weeks old female subcutaneoustumor BALB/C nude mice [4]
Doses: 1.15, 2.5, 5 mg/kg
Route of Administration: intravenous (iv) (iv)injection (through tail vein); five days (i.e. 5 injections )
Experimental Results: Demonstrated potent antitumor activity in a dose-dependent manner in xenograft mouse models.

[1]. Or CR, et al. Obatoclax, a Pan-BCL-2 Inhibitor, Targets Cyclin D1 for Degradation to Induce Antiproliferation in Human Colorectal Carcinoma Cells. Int J Mol Sci. 2016 Dec 27;18(1).
[2]. 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.
[3]. Sulkshane P, et al. BH3 mimetic Obatoclax (GX15-070) mediates mitochondrial stress predominantly via MCL-1 inhibition and induces autophagy-dependent necroptosis in human oral cancer cells. Oncotarget. 2016 Aug 5;8(36):60060-60079.
[4]. Ehrenkaufer G, et al. Identification of anisomycin, prodigiosin and obatoclax as compounds with broad-spectrum anti-parasitic activity. PLoS Negl Trop Dis. 2020 Mar 20;14(3):e0008150.

C₂₀H₁₉N₃O

317.38

803712-67-6

Obatoclax Mesylate;803712-79-0

COC1=CC(C(N2)=CC3=C2C=CC=C3)=N/C1=C\C4=C(C)C=C(C)N4

RFTSSZJZXOSICM-GRSHGNNSSA-N

InChI=1S/C20H19N3O/c1-12-8-13(2)21-16(12)10-19-20(24-3)11-18(23-19)17-9-14-6-4-5-7-15(14)22-17/h4-11,21-22H,1-3H3/b19-10-

1H-indole, 2-(2-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-

GX15-070 GX-05-070GX 15-070ObatoclaxGX05-070 GX 05-070 GX-15-070

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。