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146464-95-1结构式
146464-95-1结构式

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中文名 10-炔丙基-10-去氮杂氨基蝶呤
英文名 pralatrexate
中文别名 普拉曲沙
N-(4-(1-((2,4-二氨基-6-蝶啶)甲基)-3-丁炔基)苯甲酰基)-L-谷氨酸
英文别名 pralatrexato
pralatrexatum
10-Propargyl-10-deazaaminopterin
N-{4-[1-(2,4-Diamino-6-pteridinyl)-4-pentyn-2-yl]benzoyl}-L-glutamic acid
Folotyn
N-{4-[1-(2,4-Diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl}-L-glutamic acid
N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid
(2S)-2-[[4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl]amino]pentanedioic acid
L-Glutamic acid, N-[4-[1-[(2,4-diamino-6-pteridinyl)methyl]-3-butyn-1-yl]benzoyl]-
Pralatrexate
描述 Pralatrexate(Folotyn)是叶酸类似物,对一些细胞株的 IC50< 300 nM。
相关类别
参考文献

[1]. Foss F, Horwitz SM, Coiffier B, Bartlett N, Popplewell L, Pro B, Pinter-Brown LC, Shustov A, Furman RR, Haioun C, Koutsoukos T, O'Connor OA.,Pralatrexate Is an Effective Treatment for Relapsed or Refractory Transformed Mycosis Fungoides: A Subgroup Efficacy Analysis From the PROPEL Study,Clin Lymphoma Myeloma Leuk. 2012 Aug;12(4):238-43. Epub 2012 Apr 26.

[2]. Kelly K, Azzoli CG, Zatloukal P, Albert I, Jiang PY, Bodkin D, Pereira JR, Juhász E, Iannotti NO, Weems G, Koutsoukos T, Patel JD.,Randomized phase 2b study of pralatrexate versus erlotinib in patients with stage IIIB/IV non-small-cell lung cancer (NSCLC) after failure of prior platinum-based therapy.,J Thorac Oncol. 2012 Jun;7(6):1041-8.

[3]. Horwitz SM, Kim YH, Foss F, Zain JM, Myskowski PL, Lechowicz MJ, Fisher DC, Shustov AR, Bartlett NL, Delioukina ML, Koutsoukos T, Saunders ME, O'Connor OA, Duvic M.,Identification of an active, well-tolerated dose of pralatrexate in patients with relapsed or refractory cutaneous T-cell lymphoma.,Blood. 2012 May 3;119(18):4115-22. Epub 2012 Mar 6.

[4]. Casanova M, Medina-Pérez A, Moreno-Beltran M, Mata-Vazquez M, Rueda A.,Critical appraisal of pralatrexate in the management of difficult-to-treat peripheral T cell lymphoma.,Ther Clin Risk Manag. 2011;7:401-8. Epub 2011 Oct 7.

[5]. Hui J, Przespo E, Elefante A.,Pralatrexate: a novel synthetic antifolate for relapsed or refractory peripheral T-cell lymphoma and other potential uses.,J Oncol Pharm Pract. 2012 Jun;18(2):275-83. Epub 2011 Sep 26.

密度 1.5±0.1 g/cm3
熔点 215 °C(dec.)
分子式 C23H23N7O5
分子量 477.473
精确质量 477.176056
PSA 207.30000
LogP 0.23
外观性状 固体;White to Light yellow powder to crystal
折射率 1.704
储存条件 0-10°C;避免加热
水溶解性 水溶性:不溶;水溶解度:360 mg/l   25 °C;不溶:乙醇,氯仿
危害码 (欧洲) Xi