O-3077 Obatoclax, Methanesulfonate Salt, >99%

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 5 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 200-400 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

BAT-101

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• Obatoclax, also known as GX15-070, is a novel Bcl-2 homology domain-3 (BH3) mimetic. It occupies a hydrophobic cleft within the BH3 binding groove of Bcl-2, antagonizing Bcl-2 and thus inducing apoptosis. Chonghaile, T.N. and Letai, A. "Mimicking the BH3 domain to kill cancer cells." Oncogene 27: S149-S157 (2008).
• Obatoclax inhibited primary acute myeloid leukemia (AML) progenitor cell proliferation with an average IC50 of 0.18 ± 0.07 µM. Obatoclax potently induced apoptosis in primary AML cells with an average IC50 of 3.6 ± 1.2 µM. Konopleva, M., et al. "Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (Obatoclax)." Cancer Res. 68: 3413-3420 (2008).
• Obatoclax had a synergistic antitumor effect with the novel BH3 mimetic ABT-737 on inducing apoptosis in OCI-AML3 cells. It also had a synergistic antitumor effect with AraC (1-β-D-arabinofuranosyl cytosine) on inducing apoptosis in leukemic cell lines and primary AML samples. Konopleva, M., et al. "Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (Obatoclax)." Cancer Res. 68: 3413-3420 (2008).
• Obatoclax overcomes Bcl-2-, Bcl-xL-, Bcl-w-, and Mcl-1-mediated resistance to BAX or BAK. Obatoclax also overcomes the Mcl-1-confered resistance to the BCL-2/BCL-XL/BCL-w-selective antagonist ABT-737 and to the proteasome inhibitor bortezomib. Nguyen, M., et al. "Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis." Proc. Natl. Acad. Sci. USA 104: 19512-19517 (2007).
• Obatoclax released Bak from Mcl-1 and Bcl-xL and induced apoptosis in mantle cell lymphoma (MCL) cell lines and primary cells from patients with MCL. Obatoclax neutralized bortezomib-induced Mcl-1 accumulation and cooperated with Noxa to induce Bak displacement from this protein, and synergized with bortezomib and sensitized MCL cells to low doses of this proteasome inhibitor. Pérez-Galán, P., et al. "The BH3-mimetic GX15-070 synergizes with bortezomib in mantle cell lymphoma by enhancing Noxa-mediated activation of Bak." Blood 109: 4441-4449 (2007).
• Obatoclax augmented tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis, possibly by releasing Bak and Bim from Bcl-2/Bcl-xL or Mcl-1 proteins in human pancreatic cancer cells. Huang, S., et al. "BH3 mimetic obatoclax enhances TRAIL-mediated apoptosis in human pancreatic cancer cells." Clin. Cancer Res. 15: 150-159 (2009).
• Obatoclax inhibited influenza A virus (IAV) uptake and demonstrated broad-spectrum antiviral activity. Denisova, O.V., et al. "Obatoclax, saliphenylhalamide, and gemcitabine inhibit influenza A virus infection." J. Biol. Chem. 287: 35324-35332 (2012).
• Related CAS number: 803712-67-6 for the free base.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
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