Obatoclax mesylate (GX15-070)
(Synonyms: Obatoclax甲磺酸盐,GX15-070 Mesylate) 目录号 : GC11569
An antagonist of pro-survival Bcl-2 proteins
Cas No.:803712-79-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment: [1] | |
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Cell lines |
UMSCC-22A cells stably expressing GFP-LC3 |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
200 nM, 48 hours |
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Applications |
After the treatment, cells were fixed in 4% paraformaldehyde and then stained with Hoechst 33258. A confocal microscope was used to visualize GFP-LC3 punctate dots. Treatment of these cells for 24 or 48 h with obatoclax (100 or 200 nM) resulted in relocalization of the GFP-LC3 protein to punctate cytoplasmic dots, an indicator of autophagosome formation. Treatment with obatoclax resulted in an approximately 10-fold increase in the average number of puncta per cell at 48 h as well as 24 h. |
| nimal experiment: [2] | |
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Animal models |
Beige-nude-XID mice injected with SUDHL4 cells |
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Dosage form |
Intraperitoneal injection, 3.0 mg/kg |
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Applications |
Obatoclax (3.0 mg/kg) had little effect on tumor growth while carfilzomib (2.0 mg/kg) by itself significantly reduced tumor size. Combined treatment resulted in minimal tumor growth, an effect significantly greater than that observed with either agent alone. IVIS imaging of luciferase-expressing tumor cells confirmed the marked reduction in tumor growth with combined therapy. Kaplan-Meier analysis also demonstrated that that carfilzomib significantly increased the survival of obatoclax-treated mice. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Yazbeck VY, Li C, Grandis JR, Zang Y, Johnson DE. Single-agent obatoclax (GX15-070) potently induces apoptosis and pro-survival autophagy in head and neck squamous cell carcinoma cells. Oral Oncol. 2014 Feb;50(2):120-7. [2] Dasmahapatra G, Lembersky D, Son MP, Patel H, Peterson D, Attkisson E, Fisher RI, Friedberg JW, Dent P, Grant S. Obatoclax interacts synergistically with the irreversible proteasome inhibitor carfilzomib in GC- and ABC-DLBCL cells in vitro and in vivo. Mol Cancer Ther. 2012 May;11(5):1122-32. | |
Obatoclax mesylate, also known as GX15-070, is a hydrophobic small molecule that potently inhibits BCL-2 family by binding to the BH3-binding site of BCL-2 and other related BCL-2 family members (including BCL-XL, MCL-1, A1, and BCL-B). As a pan-BCL-2 inhibitor being investigated for the treatment of refractory malignancies, obatoclax mesylate directly induce apoptosis in cultured acute myeloid leukemia (AML) cells as well as primary patient samples and exhibits antitumor activity in mouse xengografts of solid tumor and myeloma cell lines. Study results have shown that obatoclax mesylate inhibited clonogenic growth of primary AML samples (IC50 < nmol/L) and dissociated Bak and Bim from MCL-1 in cultured AML cells.
Reference
[1].Aaron D. Schimmer, Susan O’Brien, Hagop Kantarjian, Joseph Brandwein, Bruce D. Cheson, Mark D. Minden, Karen Yee, Farhad Ravandi, Francis Giles, Andre Schuh, Vikas Gupta, Michael Andreeff, Charles Koller, Hong Chang, Suzanne Kamel-Reid, Mark Berger, Jean Viallet, and Gautam Borthakur. A phase I study of the Pan BCL-2 family inhibitor obatoclax mesylate in patients with advanced hematologic malignancies. Clin Cancer Res 2008; 14:8295-8301
| Cas No. | 803712-79-0 | SDF | |
| 别名 | Obatoclax甲磺酸盐,GX15-070 Mesylate | ||
| 化学名 | (2Z)-2-[(5Z)-5-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-4-methoxypyrrol-2-ylidene]indole;methanesulfonic acid | ||
| Canonical SMILES | CC1=CC(=C(N1)C=C2C(=CC(=C3C=C4C=CC=CC4=N3)N2)OC)C.CS(=O)(=O)O | ||
| 分子式 | C20H19N3O.CH4O3S | 分子量 | 413.5 |
| 溶解度 | ≥ 20.7 mg/mL in DMSO, ≥ 3.15 mg/mL in EtOH with ultrasonic and warming | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4184 mL | 12.0919 mL | 24.1838 mL |
| 5 mM | 0.4837 mL | 2.4184 mL | 4.8368 mL |
| 10 mM | 0.2418 mL | 1.2092 mL | 2.4184 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。