维基百科

阿利色替

化合物

阿利色替（INN：alisertib；开发代号：MLN8237），或译阿立色替、阿立塞替，是武田药品工业开发的一种口服选择性极光激酶A（英语：Aurora kinase A）抑制剂。[1]它被研究作为复发性或难治性外周T细胞淋巴瘤（英语：Peripheral T-cell lymphoma）的治疗方法。[2][3]由于临床试验结果不佳，开发于2015年被放弃。[4]

阿利色替
IUPAC名
4[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino2-methoxybenzoic acid
识别
CAS号 1028486-01-2
PubChem 24771867
ChemSpider 24700147
SMILES
 
  • COC1=C(C(=CC=C1)F)C2=NCC3=CN=C(N=C3C4=C2C=C(C=C4)Cl)NC5=CC(=C(C=C5)C(=O)O)OC
InChI
 
  • 1/C27H20ClFN4O4/c1-36-21-5-3-4-20(29)23(21)25-19-10-15(28)6-8-17(19)24-14(12-30-25)13-31-27(33-24)32-16-7-9-18(26(34)35)22(11-16)37-2/h3-11,13H,12H2,1-2H3,(H,34,35)(H,31,32,33)
InChIKey ZLHFILGSQDJULK-UHFFFAOYAB
KEGG D10085
IUPHAR配体 7790
性质
化学式 C27H20ClFN4O4
摩尔质量 518.92 g·mol−1
若非注明，所有数据均出自标准状态（25 ℃，100 kPa）下。

参考资料

  1. ^ Friedberg, JW; Mahadevan, D; Cebula, E; Persky, D; Lossos, I; Agarwal, AB; Jung, J; Burack, R; Zhou, X; Leonard, EJ; Fingert, H; Danaee, H; Bernstein, SH. Phase II study of alisertib, a selective Aurora A kinase inhibitor, in relapsed and refractory aggressive B- and T-cell non-Hodgkin lymphomas.. Journal of Clinical Oncology. Jan 1, 2014, 32 (1): 44–50. PMC 3867644  . PMID 24043741. doi:10.1200/JCO.2012.46.8793. 
  2. ^ Millennium Initiates Pivotal Phase 3 Trial of MLN8237 in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma. Takeda Pharmaceutical Company Limited; Millennium Pharmaceuticals, Inc. March 6, 2012 [20 March 2014]. 
  3. ^ Research and Development Pipeline (As of February 5, 2014) (PDF). Takeda Pharmaceutical Company Limited: 2. February 5, 2014 [20 March 2014]. 
  4. ^ Takeda Announces Termination of Alisertib Phase 3 Trial in Relapsed or Refractory Peripheral T-cell Lymphoma. 
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