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PF-06380101

Name: PF-06380101
Brand: TargetMol
SKU: T16490
Rating: 4.5 (1 reviews)

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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

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Catalog No. T16490Alias Auristatin-0101, Aur0101Cas No. 1436391-86-4

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$2,460	8-10 weeks	8-10 weeks
50 mg	$3,750	8-10 weeks	8-10 weeks
100 mg	$4,370	8-10 weeks	8-10 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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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 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

Chemical Properties

Molecular Weight	743.01
Formula	C₃₉H₆₂N₆O₆S
Cas No.	1436391-86-4
Smiles	CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)c1nccs1)OC)N(C)C(=O)[C@@H](NC(=O)C(C)(C)N)C(C)C
Relative Density.	1.143 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 65 mg/mL (87.48 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (3.36 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.3459 mL	6.7294 mL	13.4588 mL	67.2938 mL
5 mM	0.2692 mL	1.3459 mL	2.6918 mL	13.4588 mL
10 mM	0.1346 mL	0.6729 mL	1.3459 mL	6.7294 mL
20 mM	0.0673 mL	0.3365 mL	0.6729 mL	3.3647 mL
50 mM	0.0269 mL	0.1346 mL	0.2692 mL	1.3459 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc