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      Obatoclax Mesylate (GX15-070)
      Obatoclax Mesylate (GX15-070)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V0004
      CAS #: 803712-79-0Purity ≥98%

      Description: Obatoclax Mesylate (also known as GX15-070), the mesylate salt of obatoclax, is an inhibitor of Bcl-2 (B-cell leukemia protein-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, it is 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. The Bcl-2 family of proteins are overexpressed in various cancers such as the lymphatic system, breast, lung, prostate, and colon. Therefore, Obatoclax has anticancer activity as an Bcl-2 inhibitor.

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

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      Molecular Weight (MW)413.49
      FormulaC20H19N3O.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
      SynonymsGX015070; GX-015070; GX 05-070; GX 015-070; GX015-070; GX-015-070; GX 015070; GX15070MS.
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      GeneralObatoclax also exhibits high antitumor activity in SCID mice bearing human C33A cerivical carcinoma tumors at a dose of 0.5 mg/kg. 
      Animal modelFemale BALB/c or CB17 SCID/SCID mice bearing SW480, C33A, PC3, and 4T1 cells.
      FormulationObatoclax (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.
      Dosages0.0313, 0.25, 0.5 and 2 mg/kg
      AdministrationIntravenously (tail vein) once a day
      ReferencesNguyen M, et al. Proc Natl Acad Sci, 2007, 104(49), 19512-191517.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

      Obatoclax Mesylate (GX15-070)Obatoclax induces massive necrosis in mouse and human thyroid cancer cells.  2016 Jun 7;7(23):34453-71.Obatoclax Mesylate (GX15-070)Obatoclax blocks late authophagy, unrelated to cell death.  2016 Jun 7;7(23):34453-71.Obatoclax Mesylate (GX15-070) Obatoclax autofluorescence reveals its accumulation in lysosomes.  2016 Jun 7;7(23):34453-71.
      Obatoclax Mesylate (GX15-070)Obatoclax induces morphological and functional alterations in lysosomes.  2016 Jun 7;7(23):34453-71.Obatoclax Mesylate (GX15-070)Lysosomal acidic environment is critical for necrotic death induced by Obatoclax.  2016 Jun 7;7(23):34453-71.Obatoclax Mesylate (GX15-070) Mouse and human thyroid cancer cells are sensitive to lysosomal destabilization.  2016 Jun 7;7(23):34453-71.
      Obatoclax Mesylate (GX15-070) Obatoclax does not induce massive LMP, and its effect is independent of BCL2 proteins.  2016 Jun 7;7(23):34453-71.Obatoclax Mesylate (GX15-070)
      Obatoclax Mesylate (GX15-070)      		 Obatoclax Mesylate (GX15-070)

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