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Obatoclax Mesylate

Catalog No. T6275 CAS 803712-79-0

Synonyms: Obatoclax, GX15-070

Obatoclax Mesylate (GX15-070) is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3.

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Obatoclax Mesylate, CAS 803712-79-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 68.00
25 mg	In stock	$ 126.00
50 mg	In stock	$ 225.00
100 mg	In stock	$ 378.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.67%

Purity: 99.38%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Obatoclax Mesylate (GX15-070) is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3.
Targets&IC50	BCL2:220 nM (Ki, cell free)
In vitro	Obatoclax (GX15-070) potently interfered with the direct interaction between MCL-1 and BAK in intact mitochondrial outer membrane and inhibited the association between MCL-1 and BAK in intact cells [1]. Obatoclax inhibited cell growth of HL-60, U937, OCI-AML3, and KG-1 cell lines. Obatoclax induced apoptosis in AML CD34+ progenitor cells with an average IC50 of 3.59 micromol/L although clonogenicity was inhibited at concentrations of 75 to 100 nmol/L [2]. Obatoclax reduced the viability of PANC-1 and BxPC-3 cell lines and synergistically enhanced TRAIL-mediated cytotoxicity [3].
In vivo	When formulated for i.v. administration, obatoclax (2 or 3.5 mg/kg) was found to have single-agent antitumor effects in several standard mouse tumor models. Antitumor activity without animal weight loss was observed in mice bearing solid tumors [1]. Thyroid cancer-carrying [Pten,Trp53]thyr?/? mice were treated with vehicle or Obatoclax for 6 days. Live thyrocytes in Obatoclax-treated mice exhibited a dramatic reduction in Lysotracker staining [4].
Cell Research	Cells were plated in logarithmic growth phase at 2,000-4,000 cells per well in 96-well clear bottom plates and cultured for 14 to 16 h before the start of drug treatment. Serial dilutions of obatoclax or companion drug were made in DMSO, diluted 1:50 in RPMI, and then added to tissue culture media at a final concentration of 0.2% DMSO. Cells were typically treated with a dose range of compound from 50 nM to 10 mM for 72 h. Cell viability was then determined using the ViaLight kit, according to the manufacturer's instructions. To obtain percentage viability, samples are expressed as a percentage of the signal obtained from DMSO-treated cells. Dose-response points were then plotted on a log scale, and IC50 values were determined using a best-fit sigmoidal dose-response curve with variable slope. The top of the curve was set to 100% [1].
Animal Research	Cells were transplanted s.c. into the flank of female BALB/c or CB17 SCID/SCID mice (6 to 8 weeks of age) as a suspension in PBS (1.0×10^6 cells/ml, 1.5×10^6 cells/ml, 2.0×10^6 cells/ml, or 5.0×10^6 cells/ml for SW480, C33A, PC3, and 4T1 cells respectively. After 7 (SW480), 14 (C33A), or 8 (PC3 and 4T1) days, treatment with drug was initiated, and body weight and tumor size were measured three times per week. The mean relative tumor size and volume (cohort of eight animals per treatment) were calculated as follows: length (mm) ′ [width (mm)]2/2. Formulated obatoclax (tartrate salt) was administered intravenously (tail vein) once a day ′5 and cisplatin once every 3 days ′ 5 by the i.p. route. Obatoclax was formulated at the indicated concentration in 9.6% polyethylene glycol 300, 0.4% polysorbate 20, and 5% dextrose, except for the 4T1 tumor model where it was formulated at a concentration of 0.6 mg/ml in 9.48% polyethylene glycol, 0.38% polysorbate 20, 1.2 mg/ml mannitol, and 5% dextrose [1].

Synonyms	Obatoclax, GX15-070
Molecular Weight	413.49
Formula	C20H19N3O·CH4O3S
CAS No.	803712-79-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 77 mg/mL (186.2 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. 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. 2. Konopleva M, et al. Mechanisms of Antileukemic Activity of the Novel Bcl-2 Homology Domain-3 Mimetic GX15-070 (Obatoclax). Cancer Res May 1, 2008 68; 3413 3. Huang S, et al. BH3 mimetic obatoclax enhances TRAIL-mediated apoptosis in human pancreatic cancer cells. Clin Cancer Res. 2009 Jan 1;15(1):150-9. 4. Champa D, et al. Obatoclax kills anaplastic thyroid cancer cells by inducing lysosome neutralization and necrosis. Oncotarget. 2016 Jun 7;7(23):34453-71. 6. Wei WJ, et al. Obatoclax and LY3009120 Efficiently Overcome RG7204 Resistance in Differentiated Thyroid Cancer. Theranostics. 2017 Feb 23;7(4):987-1001.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Parasitic Compound Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Lung Cancer Compound Library PPI Inhibitor Library Clinical Compound Library Bioactive Compounds Library Max

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Keywords

Obatoclax Mesylate 803712-79-0 Apoptosis Autophagy Microbiology/Virology BCL Parasite Inhibitor broad-spectrum degradation BH3 anti-cancer mimetic Bcl-2 Family antiparasitic Obatoclax GX15-070 cancer colorectal proteasomal inhibit human inhibitor

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