110417-88-4

110417-88-4结构式

中文名	Dolastatin 10
英文名	L-Valinamide, N,N-dimethyl-L-valyl-N-[2-methoxy-4-[2-[1- methoxy-2-methyl-3-oxo-3-[[2-phenyl-1-(2-thiazolyl)ethyl] amino]propyl]-1-pyrrolidinyl]-1-(1-methylpropyl)-4-oxobutyl]-N-methyl-, [2S-[1[1R(R),2S],2R[1S,2S,3(R*)]]]
英文别名	D-Valinamide, N,N-dimethyl-L-valyl-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(2-thiazolyl)ethyl]amino]propyl]-1-pyrrolidinyl]-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl- N,N-Dimethyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-{[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino}propyl]-1-pyrrolidinyl}-5-methyl-1-oxo-4-heptanyl]-N-methyl-D-valinamide dolastatin 10 From dolabella auricularia (sea hare) N,N-Dimethyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-{[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino}propyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-D-valinamide

描述	Dolastatin 10 是一种有效的从海洋软体动物Dolabela auricularia中分离出来的抗有丝分裂肽,抑制微管蛋白聚合。
相关类别	信号通路 >> 抗体- 药物偶联物 >> ADC细胞毒素信号通路 >> 细胞周期/DNA损伤 >> 微管/微管蛋白信号通路 >> 细胞骨架 >> 微管/微管蛋白天然产物 >> 其他多肽产品研究领域 >> 癌症
靶点	Tubulin[1]
体外研究	Dolastatin 10是一种独特的五肽,可从海兔Dolabella auricularia中分离出来。这些体外数据与Dolastatin 10和Auristatin PE的数据非常相似,每种都具有10-5-10-6μg/ mL(10-2-10-3 nM)的GI50值,相对于人类细胞的类似微型通道线[2]。抗体-药物偶联物(ADC)包含与细胞毒性剂单甲基auristatin E(MMAE)缀合的抗CD30单克隆抗体cAC10,MMAE是微管蛋白聚合抑制剂Dolastatin 10的合成类似物[3]。
参考文献	[1]. Pitot HC, et al. Phase I trial of dolastatin-10 (NSC 376128) in patients with advanced solid tumors. Clin Cancer Res. 1999 Mar;5(3):525-31. [2]. Pettit GR, et al. Antineoplastic agents. 592. Highly effective cancer cell growth inhibitory structural modifications ofdolastatin 10. J Nat Prod. 2011 May 27;74(5):962-8. [3]. Brentuximab vedotin. Drugs R D. 2011;11(1):85-95.