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MMAF (Synonyms: Monomethylauristatin F)

Catalog No.GC10034

Anti-mitotic/anti-tubulin/antineoplastic agent

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MMAF Chemical Structure

Cas No.: 745017-94-1

Size Price Stock Qty
5mg
$72.00
In stock
10mg
$108.00
In stock
25mg
$162.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

786-O, Caki-1 and L428 cells

Preparation method

The solubility of this compound in DMSO is > 36.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

96 hrs

Applications

In 786-O, Caki-1 and L428 cells, 1F6 mAb attached by MMAF potently inhibited cell viability, with the IC50 values of 10 ng/mL, 8 ng/mL and 123 ng/mL, respectively.

Animal experiment [1]:

Animal models

Mice with 786-O RCC tumor xenografts

Dosage form

1 or 3 mg/kg; i.p.

Applications

In mice with 786-O RCC tumor xenografts, 1F6-Val-Cit-PABC-MMAF was at least 3-fold less potent than AMAsn-(D)Lys-1F6 and AW-Met-(D)Lys-1F6. Besides, compared with AMAsn-(D)Lys-1F6 and AW-Met-(D)Lys-1F6, 1F6-Val-Cit-PABC-MMAF showed lower tolerability.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Doronina SO, Bovee TD, Meyer DW, Miyamoto JB, Anderson ME, Morris-Tilden CA, Senter PD. Novel peptide linkers for highly potent antibody-auristatin conjugate. Bioconjug Chem. 2008 Oct;19(10):1960-3.

Background

MMAF is a highly potent antimitotic agent [1].

MMAF is an auristatin F (AF) derivative and is used as an antimitotic drug in the form of antibody drug conjugates (ADCs). It is reported that both the N-terminal monomethylvaline and the C-terminal carboxyl group of MMAF can be attached to the linker. Dipeptide linkers used for the attachment of MMAF to mAbs result in conjugates pronounced and potent activities against an array of tumor types. In the in vitro cytotoxicity assays, the ADC generated by attaching MMAF to the 1F6 mAb shows a potent inhibition to the cell viability with IC50 values of 10ng/ml, 8ng/ml, and 123ng/ml in 786-O, Caki-1 and L428 cell lines, respectively. Moreover, it is reported that the dipeptide linker attached to MMAF with C-terminal amino acids could modulate the efficacy, potency, and tolerability. The manipulation of the C-terminal peptide sequence leads to the improved potency, specificity and therapeutic windows of the conjugates [1].

References:
[1] Doronina SO, Bovee TD, Meyer DW, Miyamoto JB, Anderson ME, Morris-Tilden CA, Senter PD. Novel peptide linkers for highly potent antibody-auristatin conjugate. Bioconjug Chem. 2008 Oct;19(10):1960-3.

Chemical Properties

Cas No. 745017-94-1 SDF
Synonyms Monomethylauristatin F
Chemical Name (2S)-2-[[(2R,3R)-3-methoxy-3-[(2S)-1-[(3R,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid
Canonical SMILES CCC(C)C(C(CC(=O)N1CCCC1C(C(C)C(=O)NC(CC2=CC=CC=C2)C(=O)O)OC)OC)N(C)C(=O)C(C(C)C)NC(=O)C(C(C)C)NC
Formula C39H65N5O8 M.Wt 731.96
Solubility ≥ 36.6mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.3662 mL 6.831 mL 13.6619 mL
5 mM 0.2732 mL 1.3662 mL 2.7324 mL
10 mM 0.1366 mL 0.6831 mL 1.3662 mL
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 31 reference(s) in Google Scholar.)

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