1. Cell Cycle/DNA Damage Cytoskeleton Antibody-drug Conjugate/ADC Related
  2. Microtubule/Tubulin ADC Cytotoxin
  3. Auristatin E

Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids.

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

Auristatin E Chemical Structure

Auristatin E Chemical Structure

CAS No. : 160800-57-7

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids[1][2][3].

IC50 & Target

Auristatin

 

Cellular Effect
Cell Line Type Value Description References
BXPC-3 GI50
> 1.37 nM
Compound: 2a
Growth inhibition of human BxPC3 cells incubated for 48 hrs by MTT assay
Growth inhibition of human BxPC3 cells incubated for 48 hrs by MTT assay
[PMID: 28211277]
BXPC-3 GI50
> 1.37 nM
Compound: Auristatin E
Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
[PMID: 28926240]
BXPC-3 GI50
> 1.37 nM
Compound: Auristatin E
Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
Growth inhibition of human BxPC3 cells after 48 hrs by SRB assay
[PMID: 28895394]
DU-145 GI50
0.424 nM
Compound: 2a
Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay
Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay
[PMID: 28211277]
DU-145 GI50
0.424 nM
Compound: Auristatin E
Growth inhibition of human DU145 cells after 48 hrs by SRB assay
Growth inhibition of human DU145 cells after 48 hrs by SRB assay
[PMID: 28926240]
DU-145 GI50
0.424 nM
Compound: Auristatin E
Growth inhibition of human DU145 cells after 48 hrs by SRB assay
Growth inhibition of human DU145 cells after 48 hrs by SRB assay
[PMID: 28895394]
KM-20L2 GI50
0.492 nM
Compound: 2a
Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay
Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay
[PMID: 28211277]
KM-20L2 GI50
0.492 nM
Compound: Auristatin E
Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
[PMID: 28926240]
KM-20L2 GI50
0.492 nM
Compound: Auristatin E
Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay
[PMID: 28895394]
MCF7 GI50
0.232 nM
Compound: 2a
Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT assay
Growth inhibition of human MCF7 cells incubated for 48 hrs by MTT assay
[PMID: 28211277]
MCF7 GI50
0.232 nM
Compound: Auristatin E
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
[PMID: 28926240]
MCF7 GI50
0.232 nM
Compound: Auristatin E
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
[PMID: 28895394]
NCI-H460 GI50
0.533 nM
Compound: 2a
Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay
Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay
[PMID: 28211277]
NCI-H460 GI50
0.533 nM
Compound: Auristatin E
Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
[PMID: 28926240]
NCI-H460 GI50
0.533 nM
Compound: Auristatin E
Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
[PMID: 28895394]
SF-268 GI50
0.492 nM
Compound: 2a
Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay
Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay
[PMID: 28211277]
SF-268 GI50
0.492 nM
Compound: Auristatin E
Growth inhibition of human SF268 cells after 48 hrs by SRB assay
Growth inhibition of human SF268 cells after 48 hrs by SRB assay
[PMID: 28926240]
SF-268 GI50
0.492 nM
Compound: Auristatin E
Growth inhibition of human SF268 cells after 48 hrs by SRB assay
Growth inhibition of human SF268 cells after 48 hrs by SRB assay
[PMID: 28895394]
In Vitro

Auristatin E (1-10000 nM, 2 h) shows the cytotoxic effects on L2987 human lung adenocarcinoma cells and various hematologic cell lines[2].

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

In Vivo

Auristatin E (0.25 mg/kg, s.c., a single dose for 80 days) inhibits tumor growth in nude mice with subcutaneous L2987 human lung adenocarcinoma or 3396 human breast carcinoma xenografts[2].

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

Animal Model: Nude mice with subcutaneous L2987 human lung adenocarcinoma or 3396 human breast carcinoma xenografts[2]
Dosage: 0.25 mg/kg
Administration: s.c., a single dose for 80 days
Result: Showed median tumor volume when nude mice with subcutaneous L2987 human lung adenocarcinoma or 3396 human breast carcinoma xenografts were injected with conjugates or drug.
Molecular Weight

732.01

Formula

C40H69N5O7

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC(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)[C@H](C2=CC=CC=C2)O)=O)=O)OC)C)=O)C(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (136.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3661 mL 6.8305 mL 13.6610 mL
5 mM 0.2732 mL 1.3661 mL 2.7322 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.82%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3661 mL 6.8305 mL 13.6610 mL 34.1525 mL
5 mM 0.2732 mL 1.3661 mL 2.7322 mL 6.8305 mL
10 mM 0.1366 mL 0.6831 mL 1.3661 mL 3.4153 mL
15 mM 0.0911 mL 0.4554 mL 0.9107 mL 2.2768 mL
20 mM 0.0683 mL 0.3415 mL 0.6831 mL 1.7076 mL
25 mM 0.0546 mL 0.2732 mL 0.5464 mL 1.3661 mL
30 mM 0.0455 mL 0.2277 mL 0.4554 mL 1.1384 mL
40 mM 0.0342 mL 0.1708 mL 0.3415 mL 0.8538 mL
50 mM 0.0273 mL 0.1366 mL 0.2732 mL 0.6831 mL
60 mM 0.0228 mL 0.1138 mL 0.2277 mL 0.5692 mL
80 mM 0.0171 mL 0.0854 mL 0.1708 mL 0.4269 mL
100 mM 0.0137 mL 0.0683 mL 0.1366 mL 0.3415 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Auristatin E
Cat. No.:
HY-15582
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