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product name Obatoclax Mesylate (GX15-070)


Description: Obatoclax Mesylate (also known as GX15-070) is an inhibitor of Bcl-2 with Ki of 0.22 μM in a cell-free assay. Obatoclax mesylate binds 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.

References: Proc Natl Acad Sci, 2007, 104(49), 19512-191517.



Molecular Weight (MW)

413.49
Formula

C20H19N3O.CH4O3S
CAS No.

803712-79-0
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 83 mg/mL (200.7 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL
Solubility (In vivo)

30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19396548

General Obatoclax also exhibits high antitumor activity in SCID mice bearing human C33A cerivical carcinoma tumors at a dose of 0.5 mg/kg. 
Animal model Female BALB/c or CB17 SCID/SCID mice bearing SW480, C33A, PC3, and 4T1 cells.
Formulation Obatoclax (tartrate salt) is formulated in 9.6% PEG300, 0.4% polysorbate 20, and 5% dextrose; while for the 4T1 tumor model, Obatoclax is formulated  in 9.48% PEG, 0.38% polysorbate 20.
Dosages 0.0313, 0.25, 0.5 and 2 mg/kg
Administration Intravenously (tail vein) once a day
Reference Nguyen M, et al. Proc Natl Acad Sci, 2007, 104(49), 19512-191517.

Avibactam (sodium)