MMAF hydrochloride
Based on 8 publication(s) in Google Scholar
MMAF (Monomethylauristatin F) hydrochloride is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF hydrochloride is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A.
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- Purity: 99.97%
- CAS No.: 1415246-68-2
- 화학식: C39H66ClN5O8
- 분자량:768.42
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보관:
4°C, sealed storage, away from moisture
* The compound is unstable in solutions, freshly prepared is recommended.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MMAF hydrochloride
More- J Control Release. 2018 May 10;277:48-56. [Abstract]
- Mol Cancer Ther. 2023 Apr 3;22(4):459-470. [Abstract]
- Mol Ther Nucleic Acids. 2018 Mar 2;10:227-236. [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 |
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. 1415246-68-2
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Appearance Solid
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분자량 768.42
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화학식 C39H66ClN5O8
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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.Cl
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Synonyms
Monomethylauristatin F hydrochloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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 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 -
Mol Ther Nucleic Acids
2018 Mar 2;10:227-236. PMID: 29499935 -
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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용액&용해도
H2O : ≥ 100 mg/mL (130.14 mM)
DMSO : 50 mg/mL (65.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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[1].
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.
순도&문서
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 |
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| DMSO / H2O | 1 mM | 1.3014 mL | 6.5069 mL | 13.0137 mL | 32.5343 mL |
| 5 mM | 0.2603 mL | 1.3014 mL | 2.6027 mL | 6.5069 mL | |
| 10 mM | 0.1301 mL | 0.6507 mL | 1.3014 mL | 3.2534 mL | |
| 15 mM | 0.0868 mL | 0.4338 mL | 0.8676 mL | 2.1690 mL | |
| 20 mM | 0.0651 mL | 0.3253 mL | 0.6507 mL | 1.6267 mL | |
| 25 mM | 0.0521 mL | 0.2603 mL | 0.5205 mL | 1.3014 mL | |
| 30 mM | 0.0434 mL | 0.2169 mL | 0.4338 mL | 1.0845 mL | |
| 40 mM | 0.0325 mL | 0.1627 mL | 0.3253 mL | 0.8134 mL | |
| 50 mM | 0.0260 mL | 0.1301 mL | 0.2603 mL | 0.6507 mL | |
| 60 mM | 0.0217 mL | 0.1084 mL | 0.2169 mL | 0.5422 mL | |
| H2O | 80 mM | 0.0163 mL | 0.0813 mL | 0.1627 mL | 0.4067 mL |
| 100 mM | 0.0130 mL | 0.0651 mL | 0.1301 mL | 0.3253 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
MMAF hydrochloride Related Classifications
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