上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
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 Ki 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。
| 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].
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| IC50 & Target[5] |
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Bcl-2
220 nM (Ki)
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Mcl-1
1-7 μM (Ki)
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Bcl-xL
1-7 μM (Ki)
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Bcl-W
1-7 μM (Ki)
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Bcl-B
1-7 μM (Ki)
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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, 100, 150, 200, 250, 300, 350, 400, 450 nM) potently inhibits the clonogenic potential of oral cancer cells[1].
上海金畔生物科技有限公司 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. |
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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].
上海金畔生物科技有限公司 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. |
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| Clinical Trial |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 中文名称 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 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)
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| 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 (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。
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
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| 参考文献 |
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[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.
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