Art. -Nr.: HY-15162A

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MMAE-d₈

(Synonyms: Monomethyl auristatin E-d₈; Deuterated labeled MMAE)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

MMAE-d₈ is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.

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Reinheit: 99.15%
CAS. Nr.: 2070009-72-0
Formel: C₃₉H₅₉D₈N₅O₇
Molecular Weight:726.03

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years

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

MMAE-d₈ Chemical Structure

CAS. Nr.: 2070009-72-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Anwendung
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

MMAE-d₈ is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.

IC₅₀ & Target

Auristatin

Alle ADC Payloads Isoform-spezifische Produkte anzeigen :

In Vitro

Antibody-drug conjugates (ADC) comprise targeting antibodies armed with potent small-molecule payloads. ADCs are generated to target different receptors on the anaplastic large cell lymphoma line L-82, but delivered the same cytotoxic payload (monomethyl auristatin E, MMAE), and the intracellular concentration of released MMAE correlated with in vitro ADC-mediated cytotoxicity independent of target expression or drug:antibody ratios. LC-MS is used to measure the concentration of MMAE in a parallel cohort of L-82 tumors with an identical treatment regimen. Although tumor volume is not different among treatment groups 3 days after dose, the intratumoral MMAE measurement reveals two patterns. First, intratumoral MMAE concentration increases proportionally to the ADC dose, which correspondes to stronger antitumor activity. Second, the intratumoral MMAE concentration obtained from treatment with both cOKT9-vcMMAE and cAC10-vcMMAE is similar at each dose, consistent with the observation that tumor responded similarly to these two ADCs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Intratumoral MMAE concentrations consistently correlates with the extent of tumor growth inhibition in tumor xenograft models. IHC analysis reveals that nonbinding control-treated tumors consist of both CD30⁺ and CD30^-cells, presumably because they do not kill either CD30⁺ or CD30^- Karpas 299 cells. Only CD30^- cells are found in cAC10-vcMMAF-treated tumors, illustrating that cAC10-vcMMAF eliminates most CD30⁺ cells. Interestingly, the two tumors that relapses from cAC10-vcMMAE treatment are also found to be CD30^- by the end of study, indicating a small fraction of CD30^- cells might have escaped from bystander killing in these two remaining tumors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Anwendung

1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

Chemical Information

CAS. Nr. 2070009-72-0
Unlabeled Cas 474645-27-7
Appearance Solid
Molecular Weight 726.03
Formel C₃₉H₅₉D₈N₅O₇
Color White to off-white
SMILES

O=C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N1[C@H]([C@H](OC)[C@@H](C)C(N[C@H](C)[C@@H](O)C2=CC=CC=C2)=O)CCC1)=O)C)[C@@]([2H])(NC([C@@H](NC)C(C)C)=O)C([2H])(C([2H])([2H])[2H])C([2H])([2H])[2H]
Synonyms

Monomethyl auristatin E-d₈; Deuterated labeled MMAE
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years

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

Publications (10)

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Journal Impact Factor

Signal Transduct Target Ther

An aptamer-drug conjugate for promising cancer therapy with comprehensive evaluation from rodents to non-human primates. [Abstract]

2025 Sep 24;10(1):316. PMID: 40987771
J Pharm Anal

Enzyme-linked immunosorbent assays for quantification of MMAE-conjugated ADCs and total antibodies in cynomolgus monkey sera. [Abstract]

2022 Aug;12(4):645-652. PMID: 36105165
Pharmaceutics

PK/PD of Positively Charged ADC in Mice. [Abstract]

2025 Mar 17;17(3):377. PMID: 40143040
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
Drug Metab Dispos

Measurement and Mathematical Characterization of Cell-Level Pharmacokinetics of Antibody-Drug Conjugates: A Case Study with Trastuzumab-vc-MMAE. [Abstract]

2017 Nov;45(11):1120-1132. PMID: 28821484
J Pharm Biomed Anal

Development and validation of bioanalytical assays for the quantification of 9MW2821, a nectin-4-targeting antibody-drug conjugate. [Abstract]

2024 Sep 15:248:116318. PMID: 38908237
AAPS J

Quantitative Evaluation of the Effect of Antigen Expression Level on Antibody-Drug Conjugate Exposure in Solid Tumor. [Abstract]

2021 Apr 15;23(3):56. PMID: 33856579
Patent

US20220356169A1.
Patent

US20220184222A1.
Technische Universitat Darmstadt

2022 Feb.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (137.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.3774 mL

6.8868 mL

13.7735 mL

5 mM

0.2755 mL

1.3774 mL

2.7547 mL

10 mM

0.1377 mL

0.6887 mL

1.3774 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.44 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.44 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (3.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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]

Cell pellets are collected 24 hours after ADC treatment. Cell count, diameter, and circularity are determined on Vi-Cell Counter. MMAE extraction and quantification method is performed. Briefly, tumors or cell pellets are homogenized with methanol and acetonitrile containing internal standard (d⁸-MMAE for MMAE detection and ¹³C-MMAF for MMAF detection). The homogenates are centrifuged at 10,000 rpm to precipitate protein and protein-bound payloads. The supernatant is then subjected to solid phase extraction, and signals of MMAE and MMAF are detected by LC-MS^[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 (279 KB)
SDS (645 KB)
- English - EN (645 KB)
- Français - FR (645 KB)
- Deutsch - DE (645 KB)
- Norwegian - NO (645 KB)
- Español - ES (645 KB)
- Swedish - SV (645 KB)
- Italian - IT (645 KB)
- Korean - KR (645 KB)
- Portuguese - PT (645 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]. Li F, et al. Intracellular Released Payload Influences Potency and Bystander-Killing Effects of Antibody-Drug Conjugates in Preclinical Models. Cancer Res. 2016 May 1;76(9):2710-9. [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	1.3774 mL	6.8868 mL	13.7735 mL	34.4338 mL
	5 mM	0.2755 mL	1.3774 mL	2.7547 mL	6.8868 mL
	10 mM	0.1377 mL	0.6887 mL	1.3774 mL	3.4434 mL
	15 mM	0.0918 mL	0.4591 mL	0.9182 mL	2.2956 mL
	20 mM	0.0689 mL	0.3443 mL	0.6887 mL	1.7217 mL
	25 mM	0.0551 mL	0.2755 mL	0.5509 mL	1.3774 mL
	30 mM	0.0459 mL	0.2296 mL	0.4591 mL	1.1478 mL
	40 mM	0.0344 mL	0.1722 mL	0.3443 mL	0.8608 mL
	50 mM	0.0275 mL	0.1377 mL	0.2755 mL	0.6887 mL
	60 mM	0.0230 mL	0.1148 mL	0.2296 mL	0.5739 mL
	80 mM	0.0172 mL	0.0861 mL	0.1722 mL	0.4304 mL
	100 mM	0.0138 mL	0.0689 mL	0.1377 mL	0.3443 mL

Keywords

MMAE-d₈

10 Cited Publications

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MMAE-d8

Publications Citing Use of MedChemExpress (MCE) MMAE-d8

Alle ADC Payloads Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (10)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MMAE-d8 Related Classifications

HY-15162A Related Classifications

MMAE-d₈

Publications Citing Use of MedChemExpress (MCE) MMAE-d₈

MMAE-d₈ Related Classifications