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Monomethyl auristatin EAntimitotic agent

Monomethyl auristatin E

Catalog No. A3631
Size Price Stock Qty
5mg $270.00 In stock
10mg $420.00 In stock
50mg $1,122.00 In stock
100mg $1,776.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Monomethyl auristatin E

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Chemical Properties

Cas No. 474645-27-7 SDF Download SDF
Synonyms Vedotin; MMAE
Chemical Name (2S)-N-[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-3-methyl-2-(methylamino)butanamide
Canonical SMILES CCC(C)C(C(CC(=O)N1CCCC1C(C(C)C(=O)NC(C)C(C2=CC=CC=C2)O)OC)OC)N(C)C(=O)C(C(C)C)NC(=O)C(C(C)C)NC
Formula C39H67N5O7 M.Wt 717.98
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

IC50: less than 1 nM for various cancer cell lines

Monomethyl auristatin E(MMAE) is a potent antimitotic agent by blocking the polymerisation of tubulin.

Microtubules play essential role in the function of the cell. Microtubules are also reported to be involved in migration, transport and reorganization and have numerous dynamic roles including movement through motor proteins such as dynein and kinesin and the separation and segregation ofchromosomes during cell division.

In vitro: The cytotoxic effects of the MMAE conjugates on H3396 cells were determined using both pulsed and long-term drug exposure assays. It was found that under both exposure conditions, high degrees of immunological specificity were obtained with the Val-Cit conjugates. cBR96-Val-Cit-MMAE was highly active at <1/100th of the concentration required for antigen saturation [1].

In vivo: In vivo therapy tests were undertaken in athymic mice with subcutaneous L2987 human lung adenocarcinoma xenografts. MMAE conjugates were administered at 3 mg mAb component/kg/dose. All of the tested MMAE conjugates were highly efficacious, leading to long-term regressions of established tumors, whereas the nonbinding control conjugates had no effect on tumor growth. In addition, there were no apparent toxicities associated with conjugate treatment [1].

Clinical trial: In a ongoing Phase I study with platinum-resistant ovarian cancer patients, nonlinear PK of MMAE conjugate had been observed in the dose range of 0.3 to 3.2 mg/kg. Circulating CA125 results suggested no impact on the PK at 2.4 mg/kg, which was the potential clinically relevant dose. Systemic free MMAE concentration was low and consistent with other MMAE containing ADCs [2].

References:
[1] Doronina SO,Toki BE,Torgov MY,Mendelsohn BA,Cerveny CG,Chace DF,DeBlanc RL,Gearing RP,Bovee TD,Siegall CB,Francisco JA,Wahl AF,Meyer DL,Senter PD.  Development of potent monoclonal antibody auristatin conjugates for cancer therapy. Nat Biotechnol.2003 Jul;21(7):778-84.
[2] Jian Xu*, Priya Agarwal, Ola Saad, et al.  Clinical Pharmacokinetics (PK) of Anti-MUC16 Antibody-Drug Conjugates (ADCs), DMUC5754A, in Patients with Platinum-Resistant Ovarian Cancer: Results from Phase I study. This poster was presented at World ADC Summit 2014.