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PF-06380101

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Catalog No. T16490Cas No. 1436391-86-4
Alias Auristatin-0101, Aur0101

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.

PF-06380101

PF-06380101

😃Good
Catalog No. T16490Alias Auristatin-0101, Aur0101Cas No. 1436391-86-4
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 SizePriceAvailabilityQuantity
25 mg$98710-14 weeks
50 mg$1,36010-14 weeks
100 mg$1,86010-14 weeks
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Product Introduction

Bioactivity
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.
AliasAuristatin-0101, Aur0101
Chemical Properties
Molecular Weight743.01
FormulaC39H62N6O6S
Cas No.1436391-86-4
Relative Density.1.143 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.3459 mL6.7294 mL13.4588 mL67.2938 mL
5 mM0.2692 mL1.3459 mL2.6918 mL13.4588 mL
10 mM0.1346 mL0.6729 mL1.3459 mL6.7294 mL
20 mM0.0673 mL0.3365 mL0.6729 mL3.3647 mL
50 mM0.0269 mL0.1346 mL0.2692 mL1.3459 mL

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