PF-06380101

小分子

(S)-2-(2-氨基-2-甲基丙酰氨基)-N-((3R,4S,5S)-3-甲氧基-1-((S)-2-((1R,2R)-1-甲氧基-2-甲基-3-氧代-3-(((S)-2-苯基-1-(噻唑-2-基)乙基)氨基)丙基)吡咯烷-1-基)-5-甲基-1-氧代庚烷-4-基)-N,3-二甲基丁酰胺

Auristatin-0101 | Aur0101 | (S)-2-(2-Amino-2-methylpropanamido)-N-((3R,4S,5S)-3-methoxy-1-((S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((S)-2-phenyl-1-(thiazol-2-yl)ethyl)amino)propyl)pyrrolidin-1-yl)-5-methyl-1-oxoheptan-4-yl)-N,3-dimethylbutanamide | PF0

PF-06380101

P651438-5mg

5mg

Moligand™

≥98%

-20°C储存

超低温冰袋运输

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. In Vivo 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Auristatin

PF-06380101 (Aur0101) 是一种 auristatin 微管抑制剂，是具有细胞毒性的 Dolastatin 10 类似物。PF-06380101 (Aur0101)在肿瘤细胞增殖试验中表现出卓越的效力，与其他合成的乌司他丁类似物相比，它具有不同的 ADME 特性。

1436391-86-4

C39H62N6O6S

743.01 g/mol

71569947

CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@@H]([C@@H](C)C(=O)N[C@@H](CC2=CC=CC=C2)C3=NC=CS3)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)C(C)(C)N

CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@@H]([C@@H](C)C(=O)N[C@@H](CC2=CC=CC=C2)C3=NC=CS3)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)C(C)(C)N

DMSO : ≥ 65 mg/mL (87.48 mM)

3

9

19

742.445 Da

742.445 Da

184.000 Ų

52

0

1170.000

0

1

4.100