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Obatoclax mesylate (GX15-070)

Potent Bcl-2 inhibitor CAS# 803712-79-0

Obatoclax mesylate (GX15-070)

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Quality Control of Obatoclax mesylate (GX15-070)

Number of papers citing our products

Chemical structure

Obatoclax mesylate (GX15-070)

3D structure

Chemical Properties of Obatoclax mesylate (GX15-070)

Cas No. 803712-79-0 SDF Download SDF
PubChem ID 16681698 Appearance Powder
Formula C21H23N3O4S M.Wt 413.5
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Obatoclax Mesylate; GX15-070
Solubility DMSO : 12.5 mg/mL (30.23 mM; Need ultrasonic)
Chemical Name (2Z)-2-[(5Z)-5-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-4-methoxypyrrol-2-ylidene]indole;methanesulfonic acid
SMILES CC1=CC(=C(N1)C=C2C(=CC(=C3C=C4C=CC=CC4=N3)N2)OC)C.CS(=O)(=O)O
Standard InChIKey ZVAGBRFUYHSUHA-LZOXOEDVSA-N
Standard InChI InChI=1S/C20H19N3O.CH4O3S/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;1-5(2,3)4/h4-11,21,23H,1-3H3;1H3,(H,2,3,4)/b18-17-,19-10-;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Obatoclax mesylate (GX15-070)

DescriptionObatoclax (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM, can assist in overcoming MCL-1 mediated resistance to apoptosis.
TargetsBcl-2    
IC500.22 μM (Ki)    

Protocol

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.

Reacting condition

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

Application

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 (GX15-070) Dilution Calculator

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Obatoclax mesylate (GX15-070) Molarity Calculator

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Preparing Stock Solutions of Obatoclax mesylate (GX15-070)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4184 mL 12.0919 mL 24.1838 mL 48.3676 mL 60.4595 mL
5 mM 0.4837 mL 2.4184 mL 4.8368 mL 9.6735 mL 12.0919 mL
10 mM 0.2418 mL 1.2092 mL 2.4184 mL 4.8368 mL 6.0459 mL
50 mM 0.0484 mL 0.2418 mL 0.4837 mL 0.9674 mL 1.2092 mL
100 mM 0.0242 mL 0.1209 mL 0.2418 mL 0.4837 mL 0.6046 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Obatoclax mesylate (GX15-070)

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

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

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References on Obatoclax mesylate (GX15-070)

Phase I study of obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist, in patients with advanced chronic lymphocytic leukemia.[Pubmed:18931344]

Blood. 2009 Jan 8;113(2):299-305.

Obatoclax mesylate is a small molecule pan-Bcl-2 antagonist with in vitro activity against chronic lymphocytic leukemia (CLL) cells. Obatoclax was administered to patients with advanced CLL at doses ranging from 3.5 to 14 mg/m(2) as a 1-hour infusion and from 20 to 40 mg/m(2) as a 3-hour infusion every 3 weeks. Twenty-six patients received a total of 74 cycles. Dose-limiting reactions were neurologic (somnolence, euphoria, ataxia) and associated with the infusion. The maximum tolerated dose (MTD) was 28 mg/m(2) over 3 hours every 3 weeks. One (4%) of 26 patients achieved a partial response. Patients with anemia (3/11) or thrombocytopenia (4/14) experienced improvements in hemoglobin and platelet counts. Circulating lymphocyte counts were reduced in 18 of 26 patients with a median reduction of 24%. Overall, the maximum plasma concentration (C(max)) and area under the curve (AUC) values of obatoclax were dose proportional. Activation of Bax and Bak was demonstrated in peripheral blood mononuclear cells, and induction of apoptosis was related to overall obatoclax exposure, as monitored by the plasma concentration of oligonucleosomal DNA/histone complexes. Obatoclax mesylate has biologic activity and modest single-agent activity in heavily pretreated patients with advanced CLL. Further evaluation in less heavily pretreated patients and in combination with other therapeutic agents is warranted. This trial has been registered with http://clinicaltrials.gov under identifier NCT00600964.

Phase II study of obatoclax mesylate (GX15-070), a small-molecule BCL-2 family antagonist, for patients with myelofibrosis.[Pubmed:20709666]

Clin Lymphoma Myeloma Leuk. 2010 Aug;10(4):285-9.

BACKGROUND: Myelofibrosis (MF) is a disease characterized by the overexpression of the antiapoptotic BCL-2 family of proteins (eg, BCL-XL and MCL-1). PATIENTS AND METHODS: We conducted a multicenter, open-label, noncomparative phase II study of obatoclax mesylate, a small-molecule pan-BCL-2 antagonist, in patients with MF. Obatoclax was administered as a 24-hour infusion (on an outpatient basis) every 2 weeks at a fixed dose of 60 mg. RESULTS: A total of 22 patients were enrolled, with a median age of 63 years (range, 43-89 years). Twelve were men, and all 22 patients were previously treated (median of 2 previous therapies). Ten patients (45%) had a Lille score of 1, and 9 patients (41%) had a Lille score of 2. Thirteen (59%) were red blood cell transfusion dependent. A median of 7 cycles of obatoclax were administered. No patient achieved complete or partial response according to International Working Group criteria. One patient (4%) demonstrated a clinical improvement (in terms of hemoglobin and platelet count) after 7 cycles of therapy. The improvement was sustained for 4 cycles of therapy, after which he underwent allogeneic stem cell transplantation. The most common adverse events included low-grade ataxia and fatigue in 50% of the patients. Dose reduction because of toxicity was required in 1 patient, whereas 2 patients were taken off the study because of grade 3 ataxia and grade 3 heart failure. Grade 3/4 anemia and thrombocytopenia were evident in 6 (27%) and 4 (18%) patients, respectively. CONCLUSION: Obatoclax exhibits no significant clinical activity in patients with MF at the dose and schedule evaluated.

Description

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. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.

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