Monomethyl auristatin E

Modify Date: 2024-01-02 11:57:25

Monomethyl auristatin E Structure
Monomethyl auristatin E structure
Common Name Monomethyl auristatin E
CAS Number 474645-27-7 Molecular Weight 717.979
Density 1.1±0.1 g/cm3 Boiling Point 873.5±65.0 °C at 760 mmHg
Molecular Formula C39H67N5O7 Melting Point N/A
MSDS N/A Flash Point 482.1±34.3 °C

 Use of Monomethyl auristatin E


Monomethyl auristatin E (MMAE) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.

 Names

Name [3H]-Vedotin
Synonym More Synonyms

 Monomethyl auristatin E Biological Activity

Description Monomethyl auristatin E (MMAE) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
Related Catalog
Target

Microtubule[1]

In Vitro Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells[1]. MMAE sensitizes colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells[2].
In Vivo Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolongs tumor regression in xenograft models[2].
Cell Assay Monomethyl auristatin E (MMAE, 5 nM) and ionizing radiation (IR) treated cells are harvested and lysed in RIPA buffer with protease and phosphatase inhibitors. Thirty μg of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to PVDF membranes and incubated with indicated primary antibodies. Blots are developed by ECL.
Animal Admin Mice[2] 6-8 week old female athymic nu/nu mice are injected subcutaneously into thighs with 5×106 HCT-116 or PANC-1 cells in a 1:1 Matrigel and PBS solution. Mice are treated with IR or intravenous (IV) injection of ACPP-cRGD-MMAE (6 nmoles/day, 18 nmoles total, i.v.), tumor tissue is harvested, formalin fixed and paraffin embedded followed by staining with indicated antibodies. The primary antibody is used at a 1:250 dilution and is visualized using DAB as a chromagen with the UltraMap system.
References

[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.

[2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 873.5±65.0 °C at 760 mmHg
Molecular Formula C39H67N5O7
Molecular Weight 717.979
Flash Point 482.1±34.3 °C
Exact Mass 717.504028
PSA 149.54000
LogP 4.13
Vapour Pressure 0.0±0.3 mmHg at 25°C
Index of Refraction 1.519

 Synonyms

MMAE
Monomethyl auristatin E
Monomethylauristatin E
UNII-V7I58RC5EJ
monomethylauristatinE
N-Methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(1S,2R)-1-hydroxy-1-phenyl-2-propanyl]amino}-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl}-3-methoxy-5-methyl-1-oxo-4-heptanyl]-N-methyl-L-valinamide
L-Valinamide, N-methyl-L-valyl-N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-
Top Suppliers:I want be here



Get all suppliers and price by the below link:

Monomethyl auristatin E suppliers


Price: $284/10mM*1mLinDMSO

Reference only. check more Monomethyl auristatin E price