Obatoclax mesylate (GX15-070) (Synonyms: GX15070) |
Catalog No.GC11569 |
An antagonist of pro-survival Bcl-2 proteins
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 803712-79-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: [1] | |
Cell lines |
UMSCC-22A cells stably expressing GFP-LC3 |
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. |
Reaction Conditions |
200 nM, 48 hours |
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] | |
Animal models |
Beige-nude-XID mice injected with SUDHL4 cells |
Dosage form |
Intraperitoneal injection, 3.0 mg/kg |
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. |
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. |
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 | |
Synonyms | GX15070 | ||
Chemical Name | (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 | ||
Formula | C20H19N3O.CH4O3S | M.Wt | 413.5 |
Solubility | ≥ 20.7 mg/mL in DMSO, ≥ 3.15 mg/mL in EtOH with ultrasonic and warming | Storage | 4°C, protect from light |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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