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份 库存999份
| 货号： | K1015 |
| 保质期： | 2年 |
| 保存条件： | -20℃ |
| CAS号： | 803712-79-0 |
| 英文名： | Obatoclax mesylate |
| 供应商： | Kinasechem |
| 规格： | 1EA/2mg/5mg/10mg |
溶解性：DSMO 83 mg/mL Water <1 mg/ml Ethanol <1 mg/ml
纯度：>99%
描述：
Obatoclax (GX15-070), a small molecule inhibitor, can occupy a hydrophobic pocket within the BH3 binding groove of BCL-2 and induce apoptosis. Obatoclax (GX15-070) potently interfered with the direct interaction between MCL-1 and BAK in intact mitochondrial outer membrane and inhibited the association between MCL-1 and BAK in intact cells. Obatoclax potently induces apoptosis and decreases leukemia cell proliferation. GX15-070 also can inducd autophagy in esophagus cancer cell line EC9706 and osteosarcoma cancer cell line U2OS. Administration of carfilzomib and obatoclax to mice inoculated with SUDHL4 cells substantially suppressed tumor growth, activated JNK, inactivated AKT, and increased survival compared with the effects of single-agent treatment.
参考文献：
[1] Heidari N, Hicks MA, Harada H. "GX15-070 (obatoclax) overcomes glucocorticoid resistance in acute lymphoblastic leukemia through induction of apoptosis and autophagy."Cell Death Dis. 2010 Sep 16;1:e76.
[2] Dean EJ, Cummings J, Roulston A, et al."Optimization of circulating biomarkers of obatoclax-induced cell death in patients with small cell lung cancer." Neoplasia. 2011 Apr;13(4):339-47.
[3] Dasmahapatra G, Lembersky D, et al. "Obatoclax interacts synergistically with the irreversible proteasome inhibitor carfilzomib in GC- and ABC-DLBCL cells in vitro and in vivo." Mol Cancer Ther. 2012 May;11(5):1122-32.
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