Art. -Nr.: HY-15741

Mc-MMAE

(Synonyms: Maleimidocaproyl-monomethylauristatin E)

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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.

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Reinheit: 99.41%
CAS. Nr.: 863971-24-8
Formel: C₄₉H₇₈N₆O₁₀
Molecular Weight:911.18

Speicherung:

4°C, stored under nitrogen

* The compound is unstable in solutions, freshly prepared is recommended.

Mc-MMAE Chemical Structure

CAS. Nr.: 863971-24-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

IC₅₀ & Target

Auristatin

Alle Drug-Linker Conjugates for ADC Isoform-spezifische Produkte anzeigen :

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

CAS. Nr. 863971-24-8
Appearance Solid
Molecular Weight 911.18
Formel C₄₉H₇₈N₆O₁₀
Color White to light yellow
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
Synonyms

Maleimidocaproyl-monomethylauristatin E
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

* The compound is unstable in solutions, freshly prepared is recommended.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0975 mL

5.4874 mL

10.9748 mL

5 mM

0.2195 mL

1.0975 mL

2.1950 mL

10 mM

0.1097 mL

0.5487 mL

1.0975 mL

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 4.5 mg/mL (4.94 mM); Clear solution

This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Sanderson RJ, et al. In vivo drug-linker stability of an anti-CD30 dipeptide-linked auristatin immunoconjugate. Clin Cancer Res. 2005 Jan 15;11(2 Pt 1):843-52. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

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Mc-MMAE

Alle Drug-Linker Conjugates for ADC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Mc-MMAE Related Classifications

HY-15741 Related Classifications