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CAS Number: 803712-79-0
Description: 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. Obatoclax inhibited primary acute myeloid leukemia (AML) progenitor cell proliferation with an average IC50 of 0.18 ± 0.07 µM, and it potently induced apoptosis in primary AML cells with an average IC50 of 3.6 ± 1.2 µM. Obatoclax overcomes Bcl-2-, Bcl-xL-, Bcl-w-, and Mcl-1-mediated resistance to BAX or BAK and to the proteasome inhibitor bortezomib.
Format: Brown powder
Purity: ≥99%
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
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Biosafety Level: Not applicable (BSL-1)
References: 1. Chonghaile, T.N. and Letai, A. Oncogene 27: S149-S157 (2008).
2. Konopleva, M., et al. Cancer Res. 68: 3413-3420 (2008).
3. Nguyen, M., et al. Proc. Natl. Acad. Sci. USA 104: 19512-19517 (2007).
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