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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $987 | 10-14 weeks | |
50 mg | $1,360 | 10-14 weeks | |
100 mg | $1,860 | 10-14 weeks |
Description | PF-06380101 is an auristatin microtubule inhibitor and is a cytotoxic Dolastatin 10 analogue. When compared to other synthetic auristatin analogues that are used in the preparation of ADCs, PF-06380101 displays excellent potencies in tumor cell proliferat |
In vivo | PF-06380101 is considered likely to pose a low risk of causing pharmacokinetic drug interactions for drugs primarily cleared via metabolism by CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and/or CYP3A4/5 enzymes. It has been found to distribute more in human plasma than in whole blood and is identified as a P-glycoprotein (P-gp) substrate. In pharmacokinetic evaluations, PF-06380101 demonstrated a mean systemic clearance (Cl) rate of 70 mL/min/kg and a volume of distribution (Vss) of 14.70 L/kg following an intravenous (IV) dose of 20a at 20 μg/kg in Wistar Han rats. This resulted in a terminal elimination half-life (t1/2) of approximately 6 hours. The potential of new auristatin analogues, particularly 20a (PF-06380101), as antibody-drug conjugate (ADC) payloads, will be elaborated in forthcoming reports. |
Alias | Auristatin-0101, Aur0101 |
Molecular Weight | 743.01 |
Formula | C39H62N6O6S |
Cas No. | 1436391-86-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 65 mg/mL (87.48 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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