Mc-MMAE
Based on 1 Customer Validation
Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Mc-MMAE is a agent-linker conjugate for ADC.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.41%
- No. CAS: 863971-24-8
- Fòrmula: C49H78N6O10
- Peso molecular:911.18
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Almacenamiento:
4°C, stored under nitrogen
* 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
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Auristatin |
In Vitro
Synthesis of Mc-MMAE requires the addition of maleimidocaproic acid to a solution of MMAE in dichloromethane followed by the addition of diethyl cyanophosphonate and diisopropylethylamine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 863971-24-8
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Appearance Solid
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Peso molecular 911.18
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Fòrmula C49H78N6O10
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Color White to light yellow
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SMILES
O=C1N(CCCCCC(N(C)[C@H](C(N[C@@H](C(C)C)C(N([C@@H]([C@@H](C)CC)[C@@H](CC(N2[C@H]([C@H](OC)[C@H](C(N[C@@H]([C@H](C3=CC=CC=C3)O)C)=O)C)CCC2)=O)OC)C)=O)=O)C(C)C)=O)C(C=C1)=O
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Synonyms
Maleimidocaproyl-monomethylauristatin E
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
Solvente y solubilidad
In Vitro:
DMSO : 180 mg/mL (197.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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)
In Vivo:
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: 4.5 mg/mL (4.94 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 4.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 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.
In Vivo Dissolution Calculator
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.
Protocolo
Kinase Assay[1]
Horseradish peroxidase (HRP) is thiolated with 2-iminothiolane and conjugated to mc-MMAE to generate the HRP-MMAE reporter enzyme-drug conjugate. Briefly, a thiolation reaction mixture containing 0.2 mM HRP (8 mg/mL) and 50 mM 2-iminothiolane in 25 mM sodium borate decahydrate (Na2B4O7•10H2O) buffer (pH 9.0) is incubated for 1 hour at 37°C. Unreacted 2-iminothiolane is removed by passage through a PD-10 desalting column equilibrated in PBS (pH 7.4). Peak fractions are pooled and mc-MMAE is coupled to thiolated HRP (HRP-SH) at a molar ratio of 3:1. The final conjugation reaction mixture contained 80 μM HRP-SH (3.2 mg/mL) in sodium borate buffer [50 mM H3BO3, 50 mM NaCl (pH 8.0); 80% v/v] and 240 μM mc-MMAE in ice-cold CH3CN (20% v/v). After 30 minutes on ice, the reaction is terminated with a 20-fold molar excess of free cysteine (4.8 mM) before PD-10 chromatography. Peak fractions containing HRP-MMAE (exchanged into PBS) are pooled and evaluated for extent of modification using the thiol-reactive dye, Alexa Fluor 594 C5 maleimide[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (272 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 1.0975 mL | 5.4874 mL | 10.9748 mL | 27.4370 mL |
| 5 mM | 0.2195 mL | 1.0975 mL | 2.1950 mL | 5.4874 mL | |
| 10 mM | 0.1097 mL | 0.5487 mL | 1.0975 mL | 2.7437 mL | |
| 15 mM | 0.0732 mL | 0.3658 mL | 0.7317 mL | 1.8291 mL | |
| 20 mM | 0.0549 mL | 0.2744 mL | 0.5487 mL | 1.3718 mL | |
| 25 mM | 0.0439 mL | 0.2195 mL | 0.4390 mL | 1.0975 mL | |
| 30 mM | 0.0366 mL | 0.1829 mL | 0.3658 mL | 0.9146 mL | |
| 40 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6859 mL | |
| 50 mM | 0.0219 mL | 0.1097 mL | 0.2195 mL | 0.5487 mL | |
| 60 mM | 0.0183 mL | 0.0915 mL | 0.1829 mL | 0.4573 mL | |
| 80 mM | 0.0137 mL | 0.0686 mL | 0.1372 mL | 0.3430 mL | |
| 100 mM | 0.0110 mL | 0.0549 mL | 0.1097 mL | 0.2744 mL |
Mc-MMAE Related Classifications
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