产品
编 号：F163016
分子式：C39H62N6O6S
分子量：743.01
分子式：C39H62N6O6S
分子量：743.01
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 1436391-86-4
产品详情
生物活性：
PF-06380101 (Aur0101), an auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue. PF-06380101 (Aur0101) shows excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.
体内研究：
After an IV dose of 20a at 20 μg/kg to Wistar Han rats, PF-06380101 exhibited a mean systemic clearance (Cl) of 70 mL/min/kg and a volume of distribution (Vss) of 14.70 L/kg, resulting in a terminal elimination half-life (t1/2) of approximately 6 h. PF-06380101 preferentially distributes into human plasma relative to whole blood and that PF-06380101 is a P-glycoprotein (P-gp) substrate. PF-06380101 is anticipated to be of low risk to perpetrate pharmacokinetic drug interactions with compounds for which CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and/or CYP3A4/5-mediated metabolism constitutes the primary mechanism of clearance. The utility of the new auristatin analogues as ADC payloads including the development of the lead analogue 20a (PF-06380101) will be reported in due course.
PF-06380101 (Aur0101), an auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue. PF-06380101 (Aur0101) shows excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.
体内研究：
After an IV dose of 20a at 20 μg/kg to Wistar Han rats, PF-06380101 exhibited a mean systemic clearance (Cl) of 70 mL/min/kg and a volume of distribution (Vss) of 14.70 L/kg, resulting in a terminal elimination half-life (t1/2) of approximately 6 h. PF-06380101 preferentially distributes into human plasma relative to whole blood and that PF-06380101 is a P-glycoprotein (P-gp) substrate. PF-06380101 is anticipated to be of low risk to perpetrate pharmacokinetic drug interactions with compounds for which CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and/or CYP3A4/5-mediated metabolism constitutes the primary mechanism of clearance. The utility of the new auristatin analogues as ADC payloads including the development of the lead analogue 20a (PF-06380101) will be reported in due course.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备