auristatin F;;;; Auristatin F;Auristantin F;N,N-Dimethyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(1S)-1-carboxy-2-phenylethyl]amino}-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl}-3-methoxy-5-methyl-1-oxo-4-heptanyl]-N-methyl-L-valinamide;Auristatin F;CS-1370;Auristatin F TFA Salt;L-Phenylalanine, N,N-dimethyl-L-valyl-L-valyl-(3R,4S,5S)-3-methoxy-5-methyl-4-(methylamino)heptanoyl-(αR,βR,2S)-β-methoxy-α-methyl-2-pyrrolidinepropanoyl-;Auristatin F (AF);(S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((S)-2-(Dimethylamino)-3-methylbutanamido)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid
Cas No.
163768-50-1
分子式
C40H67N5O8
分子量
745.99
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Auristatin F 是抗体偶联药物中一种有效的细胞毒素 (cytotoxin),也是 MMAF 的类似物。Auristatin F 是一种有效的微管 (microtubule) 抑制剂和血管损伤剂 (VDA)。Auristatin F 通过阻止微管蛋白聚集抑制细胞分裂。Auristatin F 可用于抗体-药物偶联物 (ADC)。
生物活性
Auristatin F is a potent cytotoxin in antibo-conjugated drugs and an analogue of MMAF. Auristatin F is a potent microtubule inhibitor and vascular damaging agent (VDA). Auristatin F inhibits cell division by preventing tubulin aggregation.Auristatin F can be used in antibody-drug conjugates (ADC) .
性状
Solid
IC50 & Target[1][2]
Microtubule
体外研究(In Vitro)
Auristatin F and Monomethyl Auristatin F (MMAF) are potent ADC cytotoxin used in antibody-drug conjugates. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Auristatin F (5 mg/kg; i.v.; male Sprague-Dawley rats) has C max of 8276.76 ng/mL. The AUC last is 65661.30 min*ng/mL, and the clearance (CL) is 77.33 mL/min/kg, which is above the hepatic blood flow in the rat. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Roy S, et al. SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth. Chem Commun (Camb). 2017 Apr 11;53(30):4234-4237.[2]. Park MH, et, al. Pharmacokinetic and Metabolism Studies of Monomethyl Auristatin F via Liquid Chromatography-Quadrupole-Time-of-Flight Mass Spectrometry. Molecules. 2019 Jul 29;24(15):2754.
溶解度数据
In Vitro: DMSO : 200 mg/mL (268.10 mM; Need ultrasonic)配制储备液