| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P651438-5mg |
5mg |
期货  |
| |
| P651438-10mg |
10mg |
期货 |
|
| 别名 | (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 |
|---|---|
| 英文别名 | 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 |
| 规格或纯度 | Moligand™, ≥98% |
| 英文名称 | PF-06380101 |
| 生化机理 | 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。 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 产品介绍 |
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 |
| 纯度 | ≥98% |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | 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 |
| 分子量 | 743.01 |
| 溶解性 | DMSO : ≥ 65 mg/mL (87.48 mM) |
|---|---|
| 分子量 | 743.000 g/mol |
| XLogP3 | 4.100 |
| 氢键供体数Hydrogen Bond Donor Count | 3 |
| 氢键受体数Hydrogen Bond Acceptor Count | 9 |
| 可旋转键计数Rotatable Bond Count | 19 |
| 精确质量Exact Mass | 742.445 Da |
| 单同位素质量Monoisotopic Mass | 742.445 Da |
| 拓扑极表面积Topological Polar Surface Area | 184.000 Ų |
| 重原子数Heavy Atom Count | 52 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 1170.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 8 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
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