[CAS NO. 163768-50-1]  AuristatinF

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PRODUCTS SPECIFICATIONS [163768-50-1]

Distributor
Catalog
AS901825
Brand
Arctom Scientific
CAS
163768-50-1

DESCRIPTION [163768-50-1]

Overview

MDLMFCD25976745
Molecular Weight745.99
Molecular FormulaC40H67N5O8
SMILESCC(C)[C@H](N(C)C)C(N[C@H](C(N([C@@H]([C@@H](C)CC)[C@@H](CC(N1CCC[C@@]1([H])[C@H](OC)[C@@H](C)C(N[C@H](C(O)=O)CC2=CC=CC=C2)=O)=O)OC)C)=O)C(C)C)=O

For research use only. We do not sell to patients.

Summary

Auristatin F is a potent cytotoxin in antibo-conjugated drugs and an analogue of MMAF. Auristatin F is a potent microtubule inhibitor and vascular damaging agent (VDA). Auristatin F inhibits cell division by preventing tubulin aggregation. Auristatin F can be used in antibody-drug conjugates (ADC) [1] [2] .


IC50 & Target

Microtubule [1]


In Vitro

Auristatin F and Monomethyl Auristatin F (MMAF) are potent ADC cytotoxin used in antibody-drug conjugates [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

Auristatin F (5 mg/kg; i.v.; male Sprague-Dawley rats) has C max of 8276.76 ng/mL. The AUC last is 65661.30 min*ng/mL, and the clearance (CL) is 77.33 mL/min/kg, which is above the hepatic blood flow in the rat [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats [2]
Dosage: 5 mg/kg
Administration: Intravenous injection
Result: 1.19
Parameter
Dose (i.v.) mg/kg 5
C max (ng/mL) 8276.76
AUC last (min*ng/mL) 62661.30
CL (mL/min/ng) 77.33
Vss (mL/Kg) 1057.13

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years

* The compound is unstable in solutions, freshly prepared is recommended.


Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL ( 268.10 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3405 mL 6.7025 mL 13.4050 mL
5 mM 0.2681 mL 1.3405 mL 2.6810 mL
10 mM 0.1341 mL 0.6703 mL 1.3405 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 5 mg/mL (6.70 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (6.70 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 5 mg/mL (6.70 mM); Clear solution

* All of the co-solvents are available by MCE.