4,9-二氢-1-(2-甲氧基乙基)-2-甲基-4,9-二氧代-3-(2-吡嗪甲基)-1H-萘并[2,3-D]咪唑溴化物

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4,9-二氢-1-(2-甲氧基乙基)-2-甲基-4,9-二氧代-3-(2-吡嗪甲基)-1H-萘并[2,3-D]咪唑溴化物

4,9-二氢-1-(2-甲氧基乙基)-2-甲基-4,9-二氧代-3-(2-吡嗪甲基)-1H-萘并[2,3-D]咪唑溴化物

编号ABP000261 化学名称YM155/YM-155 CAS781661-94-7 MDL: MFCD11983133 分子式C20H19N4O3.Br 分子量443.299 纯度 >99%

化学名称 : 4,9-二氢-1-(2-甲氧基乙基)-2-甲基-4,9-二氧代-3-(2-吡嗪甲基)-1H-萘并[2,3-D]咪唑溴化物

CAS : 781661-94-7

英文名称: YM155/YM-155

英文同义词: YM155

溶解度:DMSO

储存条件:at -20C 2 years

生物活性

YM155, a novel small molecule survivin inhibitor, suppressed expression of survivin and induced apoptosis in PC-3 and PPC-1 human HRPC cell lines at 10 nmol/L. In a s.c.xenogr afted PC-3 tumor model in mice, 3-day continuous infusions of YM155 at 3 to 10 mg/kg induced massive tumor regression accompanied by suppression of intratumoral survivin.Pharmacokinetic analyses indicated that YM155 is highly distributed to tumors and at concentrations f20-fold higher than those in plasma.

参考文献

1. Nakahara T, Takeuchi M, Kinoyama I, Minematsu T, Shirasuna K, Matsuhisa A, Kita A, Tominaga F, Yamanaka K, Kudoh M, Sasamata M. YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts. Cancer Res. 2007 Sep 1;67(17):8014-21. 2. Tolcher AW, Mita A, Lewis LD, Garrett CR, Till E, Daud AI, Patnaik A, Papadopoulos K, Takimoto C, Bartels P, Keating A, Antonia S. Phase I and pharmacokinetic study of YM155, a small-molecule inhibitor of survivin. J Clin Oncol. 2008 Nov 10;26(32):5198-203. Epub 2008 Sep 29. 3. Iwasa T, Okamoto I, Suzuki M, Nakahara T, Yamanaka K, Hatashita E, Yamada Y, Fukuoka M, Ono K, Nakagawa K. Radiosensitizing effect of YM155, a novel small-molecule survivin suppressant, in non-small cell lung cancer cell lines. Clin Cancer Res. 2008 Oct 15;14(20):6496-504. 4. Satoh T, Okamoto I, Miyazaki M, Morinaga R, Tsuya A, Hasegawa Y, Terashima M, Ueda S, Fukuoka M, Ariyoshi Y, Saito T, Masuda N, Watanabe H, Taguchi T, Kakihara T, Aoyama Y, Hashimoto Y, Nakagawa K. Phase I study of YM155, a novel survivin suppressant, in patients with advanced solid tumors. Clin Cancer Res. 2009 Jun 1;15(11):3872-80. Epub 2009 May 26. 5. Giaccone G, Zatloukal P, Roubec J, Floor K, Musil J, Kuta M, van Klaveren RJ, Chaudhary S, Gunther A, Shamsili S. Multicenter phase II trial of YM155, a small-molecule suppressor of survivin, in patients with advanced, refractory, non-small-cell lung cancer. J Clin Oncol. 2009 Sep 20;27(27):4481-6. Epub 2009 Aug 17.

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