Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 proliferation assays and differential ADME properties.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 987.00 | |
50 mg | 10-14 weeks | $ 1,360.00 | |
100 mg | 10-14 weeks | $ 1,860.00 |
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 proliferation assays and differential ADME properties. |
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. |
Synonyms | Auristatin-0101, Aur0101 |
Molecular Weight | 743.01 |
Formula | C39H62N6O6S |
CAS No. | 1436391-86-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 65 mg/mL (87.48 mM)
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PF-06380101 1436391-86-4 Others PF 06380101 Auristatin-0101 PF06380101 Aur0101 inhibitor inhibit