2. Cell Cycle/DNA Damage Cytoskeleton Antibody-drug Conjugate/ADC Related
  3. Microtubule/Tubulin ADC Cytotoxin
  4. MMAE-d8

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

Cat. No.: HY-15162A Purity: 99.15%
COA Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

MMAE-d<sub>8</sub> Chemical Structure

MMAE-d8 Chemical Structure

CAS No. : 2070009-72-0

Size Price Stock Quantity
1 mg USD 1320 In-stock
1 mg * 5 USD 3000 In-stock
1 mg * 10 USD 5690 In-stock
5 mg   Get quote  
10 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of MMAE-d8:

MMAE-d8 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

Auristatin

 

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.

MMAE-d8 Related Antibodies
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.
Molecular Weight

726.03

Formula

C39H59D8N5O7
CAS No.
Unlabeled CAS

474645-27-7
Appearance

Solid

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]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3774 mL 6.8868 mL 13.7735 mL
5 mM 0.2755 mL 1.3774 mL 2.7547 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.29%

COA (254 KB) RP-HPLC (117 KB)

Handling Instructions (2659 KB)
References
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].

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

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
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MMAE-d8 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MMAE-d82070009-72-0Monomethyl auristatin E-d8Deuterated labeled MMAEMicrotubule/TubulinADC CytotoxinADC PayloadInhibitorinhibitorinhibit

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