MMAF
Based on 8 publication(s) in Google Scholar
MMAF (Monomethylauristatin F) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin and SGN-CD19A.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 745017-94-1
- Formula: C39H65N5O8
- Molecular Weight:731.96
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Storage:
4°C, sealed storage, away from moisture
* The compound is unstable in solutions, freshly prepared is recommended.
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MMAF
More- J Control Release. 2018 May 10;277:48-56. [Abstract]
- Mol Ther Nucleic Acids. 2018 Mar 2;10:227-236. [Abstract]
- Mol Cancer Ther. 2023 Apr 3;22(4):459-470. [Abstract]
- Target Oncol. 2019 Oct;14(5):577-590. [Abstract]
- Oncol Rep. 2021 Feb;45(2):776-785. [Abstract]
- Research Square Preprint. 2023 Dec 4.
- University of Minnesota. 2022 Sep.
- Patent. US20210393733A1.
Biological Activity
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Auristatin |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | GI50 |
0.24 nM
Compound: 6-OMe, MMAF-OMe
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Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay
Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay
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[PMID: 25431858] |
| BT-474 | IC50 |
8.8 nM
Compound: MMAF
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Cytotoxicity against human BT-474 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay
Cytotoxicity against human BT-474 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay
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[PMID: 34676042] |
| H3396 | IC50 |
105 nM
Compound: 39; MMAF
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Cytotoxicity against human H3396 cells assessed as cell growth inhibition
Cytotoxicity against human H3396 cells assessed as cell growth inhibition
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[PMID: 35072477] |
| H3396 | IC50 |
105 nM
Compound: 4; MMAF
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Cytotoxicity against human H3396 cells assessed as inhibition of cell growth incubated for 96 hrs by Alamar blue assay
Cytotoxicity against human H3396 cells assessed as inhibition of cell growth incubated for 96 hrs by Alamar blue assay
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[PMID: 39068862] |
| HCT-116 | IC50 |
2.88 μM
Compound: 39; MMAF
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Cytotoxicity against human HCT-116 cells assessed as reduction inc cell viability
Cytotoxicity against human HCT-116 cells assessed as reduction inc cell viability
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[PMID: 35072477] |
| HL-60 | IC50 |
137 nM
Compound: 39; MMAF
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Cytotoxicity against P-gp negative human HL-60 cells assessed as reduction inc cell viability
Cytotoxicity against P-gp negative human HL-60 cells assessed as reduction inc cell viability
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[PMID: 35072477] |
| HT-29 | IC50 |
10 nM
Compound: 39; MMAF
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Cytotoxicity against human HT-29 cells assessed as cell growth inhibition
Cytotoxicity against human HT-29 cells assessed as cell growth inhibition
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[PMID: 35072477] |
| MDA-MB-361 | GI50 |
0.21 nM
Compound: 6-OMe, MMAF-OMe
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Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay
Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay
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[PMID: 25431858] |
| NCI-N87 | GI50 |
0.44 nM
Compound: 6-OMe, MMAF-OMe
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Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay
Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay
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[PMID: 25431858] |
| SK-BR-3 | IC50 |
5.3 nM
Compound: MMAF
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Cytotoxicity against human SKBR3 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay
Cytotoxicity against human SKBR3 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay
|
[PMID: 34676042] |
MMAF inhibits anaplastic large cell lymphoma Karpas 299, breast carcinoma H3396, renal cell carcinoma 786-O and Caki-1 cells with IC50s of 119, 105, 257 and 200 nM in vitro cytotoxicity assay[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 745017-94-1
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Appearance Solid
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Molecular Weight 731.96
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Formula C39H65N5O8
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Color White to off-white
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SMILES
CC(C)[C@H](NC)C(N[C@H](C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N1CCC[C@@]1([H])[C@H](OC)[C@@H](C)C(N[C@H](C(O)=O)CC2=CC=CC=C2)=O)=O)C)=O)C(C)C)=O
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Synonyms
Monomethylauristatin F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* The compound is unstable in solutions, freshly prepared is recommended.
Publications (8)
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Journal Impact Factor
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Most Recent
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J Control Release
EV20-mediated delivery of cytotoxic auristatin MMAF exhibits potent therapeutic efficacy in cutaneous melanoma. [Abstract]2018 May 10;277:48-56. PMID: 29550398 -
Mol Ther Nucleic Acids
2018 Mar 2;10:227-236. PMID: 29499935 -
Mol Cancer Ther
Payload-binding Fab fragments increase the therapeutic index of MMAE antibody-drug conjugates. [Abstract]2023 Apr 3;22(4):459-470. PMID: 36723609 -
Target Oncol
Therapeutic Targeting of Golgi Phosphoprotein 2 (GOLPH2) with Armed Antibodies: A Preclinical Study of Anti-GOLPH2 Antibody Drug Conjugates in Lung and Colorectal Cancer Models of Patient Derived Xenografts (PDX). [Abstract]2019 Oct;14(5):577-590. PMID: 31541350 -
Oncol Rep
EV20‑sss‑vc/MMAF, an HER‑3 targeting antibody‑drug conjugate displays antitumor activity in liver cancer. [Abstract]2021 Feb;45(2):776-785. PMID: 33416143 -
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Solvent & Solubility
DMSO : 140 mg/mL (191.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.5 mg/mL (4.78 mM); Clear solution
This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * The compound is unstable in solutions, freshly prepared is recommended.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cells are treated with serial dilutions of test molecules and incubated 4-6 days depending on cell line. Assessment of cellular growth and data reduction to generate IC50 values is done using Alamar Blue dye reduction assay[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: When subcutaneous Karpas 299 tumor size reaches 300 mm3, three animals per group receives one injection of 10 mg antibody component/kg body weight of either cAC10-L1-MMAF4 or cBR96-L1-MMAF4 intravenously. Tumors are then removed and placed in optimal cutting temperature compound, and 5 μm-thin frozen tissue sections are stained using immunohistochemistry evaluation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Lee JW, et al. EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70. [Content Brief]
[2]. Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4. [Content Brief]
[3]. Kim EG, et al. Strategies and Advancement in Antibody-Drug Conjugate Optimization for Targeted CancerTherapeutics. [Content Brief]
[4]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24. [Content Brief]
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 | 1.3662 mL | 6.8310 mL | 13.6619 mL | 34.1549 mL |
| 5 mM | 0.2732 mL | 1.3662 mL | 2.7324 mL | 6.8310 mL | |
| 10 mM | 0.1366 mL | 0.6831 mL | 1.3662 mL | 3.4155 mL | |
| 15 mM | 0.0911 mL | 0.4554 mL | 0.9108 mL | 2.2770 mL | |
| 20 mM | 0.0683 mL | 0.3415 mL | 0.6831 mL | 1.7077 mL | |
| 25 mM | 0.0546 mL | 0.2732 mL | 0.5465 mL | 1.3662 mL | |
| 30 mM | 0.0455 mL | 0.2277 mL | 0.4554 mL | 1.1385 mL | |
| 40 mM | 0.0342 mL | 0.1708 mL | 0.3415 mL | 0.8539 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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