CAS: 1001600-56-1; (2S,2'S)-N,N'-((2S,2'S)-(Hexane-1,6-Diylbis(Azanediyl))Bis(1-Oxo-3,3-Diphenylpropane-1,2-Diyl))Bis(1-((S)-2-Cyclohexyl-2-((S)-2-(Methylamino)Propanamido)Acetyl)Pyrrolidine-2-Carboxamide)
- 英文名称(2S,2'S)-N,N'-((2S,2'S)-(Hexane-1,6-Diylbis(Azanediyl))Bis(1-Oxo-3,3-Diphenylpropane-1,2-Diyl))Bis(1-((S)-2-Cyclohexyl-2-((S)-2-(Methylamino)Propanamido)Acetyl)Pyrrolidine-2-Carboxamide)
- 中文名称(2S,2'S)-N,N'-((2S,2'S)-(己烷-1,6-二基双(氮杂二基))双(1-氧代-3,3-二苯基丙烷-1,2-二基))双(1-((S)-2-环己基-2-((S)-2-(甲基氨基)丙酰胺基)乙酰)吡咯烷-2-甲酰胺)
- IUPAC名称(2S,2'S)-N,N'-((2S,2'S)-(hexane-1,6-diylbis(azanediyl))bis(1-oxo-3,3-diphenylpropane-1,2-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide)
- 其它别名Bv6
- CAS编号1001600-56-1
- MFCD编号:MFCD28168021
- 分子式:C70H96N10O8分子量:1205.6
- 产品CID: 5566
物理性质
- 沸点1376.7±65.0 °C(预测)
- 密度1.177±0.06 g/cm3(预测)
- pKa:12.89±0.20(预测)
- PSA:239.28
- LogP:9.744
- 溶解性≥60.28 mg/mL In DMSO; Insoluble In H2O; ≥12.6 mg/mL In Etoh With Ultrasonic
- 外观形态白色至类白色固体
- 储存条件请置于阴暗处, 惰性气氛中,冷冻保存, 低于 -20°C
- 产品应用该化合物是一种SMAC 放大器,是CPAP和XAAP的双重抑制器.它抑制了HCC193 NSCCLC细胞在体外(IC50=7.2微克M)的活性,在HCC 193和H460细胞线中诱发了吸附性硬化症,通过激活切开的CASPASE-8和CASPASASE-9,大大加强了这些细胞线的放射敏化.BV-6在不成熟的登地细胞中中中点激活了NF-B路径,它加强了CIK细胞在血性恶性肿瘤(H9,THHP-1和TANOUE)和固态肿瘤(RH1,RHF30和TE671). BV-6还促进了外围血液单核细胞中的聚性硬性反应,并大大抑制了免疫细胞的细胞的胆毒潜能.在VIVO,BV6-6治疗四周内降低了植入细胞的上和压力细胞的表象细胞的表达水平,减少了其面积,重量和面积的百分比.
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主要参考文献
1: Schmidt N, Haydn T, Schneider I, Busch H, Boerries M, Fulda S. Smac mimetic induces an early wave of gene expression via NF-κB and AP-1 and a second wave via TNFR1 signaling. Cancer Lett. 2018 Feb 5. pii: S0304-3835(18)30123-X. doi: 10.1016/j.canlet.2018.01.082. [Epub ahead of print] doi: 10.1016/j.canlet.2017.09.002. Epub 2017 Sep 18. doi: 10.1016/j.canlet.2017.07.008. Epub 2017 Jul 14. doi: 10.1080/1061186X.2017.1339192. Epub 2017 Jul 11. doi: 10.3389/fimmu.2017.00202. eCollection 2017.
6: Siegmund D, Kums J, Ehrenschwender M, Wajant H. Activation of TNFR2 sensitizes macrophages for TNFR1-mediated necroptosis. Cell Death Dis. 2016 Sep 22;7(9):e2375. doi: 10.1038/cddis.2016.285.
7: Safferthal C, Rohde K, Fulda S. Therapeutic targeting of necroptosis by Smac mimetic bypasses apoptosis resistance in acute myeloid leukemia cells. Oncogene. 2017 Mar;36(11):1487-1502. doi: 10.1038/onc.2016.310. Epub 2016 Nov 21. doi: 10.1038/cdd.2016.102. Epub 2016 Nov 11.
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