803712-79-0

Basic information

• Product Name: Obatoclax mesilate
• Synonyms: OBATOCLAX MESYLATE;2-[2-[(3,5-Dimethyl-1H-pyrrol-2-yl)methylene]-3-methoxy-2H-pyrrol-5-yl]-1H-indole methanesulfonate;Obatoclax mesilate;1H-Indole, 2-(2-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-3-methoxy-2H-pyrrol-5-yl)-, monomethanesulfonate;Gx 15-070;Gx 15-070ms;Gx015-070;Unii-39200fj43j
• CAS NO: 803712-79-0
• Molecular Formula: C20H19N3O.CH4O3S
• Molecular Weight: 413.49
• EINECS: 1592732-453-0
• Product Categories: Inhibitor;Inhibitors
• Mol File: 803712-79-0.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Storage Temp.: -20°C
• Solubility: Soluble in DMSO (up to 5 mg/ml).
• Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
• CAS DataBase Reference: Obatoclax mesilate(CAS DataBase Reference)
• NIST Chemistry Reference: Obatoclax mesilate(803712-79-0)
• EPA Substance Registry System: Obatoclax mesilate(803712-79-0)

Safety Data

• Hazardous Substances Data: 803712-79-0(Hazardous Substances Data)

Usage

Description

Obatoclax mesilate, also known as GX15-070, is a novel Bcl-2 homology domain-3 (BH3) mimetic with the chemical formula 803712-79-0. It is a red powder that inhibits primary acute myeloid leukemia (AML) progenitor cell proliferation and induces apoptosis in primary AML cells. Obatoclax mesilate is an inhibitor of Bcl-2 with a Ki of 0.22 μM and has the potential to synergize with other agents in cytotoxicity against a variety of cancer cells.

Uses

Used in Oncology:
Obatoclax mesilate is used as an anticancer agent for its ability to inhibit Bcl-2, a protein that plays a crucial role in the regulation of apoptosis. It is particularly effective in targeting primary acute myeloid leukemia (AML) progenitor cells, with an IC50 of 0.18 μM for proliferation inhibition and 3.6 μM for inducing apoptosis.
Used in Combination Therapy:
Obatoclax mesilate is used in combination therapy with other agents, such as chloroquine and cytarabine, to enhance cytotoxicity against a variety of cancer cells. This synergistic effect allows for more effective treatment strategies and improved patient outcomes.
Used in Drug Development:
As a novel BH3 mimetic, Obatoclax mesilate serves as a valuable compound in the development of new drugs targeting Bcl-2 and its associated pathways. Its unique properties and potential synergistic effects with other agents make it a promising candidate for further research and development in the field of oncology.

References

1) Chonghaile and Letai (2008),?Mimicking the BH3 domain to kill cancer cells; Oncogene,?27?S149 2) Konopleva?et al. (2008),?Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax); Cancer Res.,?68?3413 3) Wang?et al. (2014),?Combination of chloroquine and GX15-070 (obatoclax) results in synergistic cytotoxicity against pancreatic cancer cells; Oncol. Rep.,?32?2789 4) Xie?et al. (2015),?Obatoclax potentiates the cytotoxic effect of cytarabine on acute myeloid leukemia cells by enhancing DNA damage; Mol. Oncol.,?9?409

InChI:InChI=1/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/h4-11,21-22H,1-3H3;1H3,(H,2,3,4)/b19-10-;