1. Cell Cycle/DNA Damage Cytoskeleton Antibody-drug Conjugate/ADC Related
  2. Microtubule/Tubulin ADC Cytotoxin
  3. S-methyl DM1

S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects.

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

S-methyl DM1 Chemical Structure

S-methyl DM1 Chemical Structure

CAS No. : 912569-84-7

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1 mg USD 250 In-stock
5 mg USD 750 In-stock
10 mg USD 1280 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects[1][2].

IC50 & Target[1]

Maytansinoids

 

In Vitro

S-methyl DM1 is the primary cellular or liver metabolite of antibody-maytansinoid conjugates prepared with thiol-containing maytansinoids DM1[1].
The half-maximal concentration for inhibition of microtubule assembly for for S-methyl DM1 is 4 μM. At 100 nM S-methyl-DM1 (84%) suppresses dynamic instability more strongly than Maytansine (45%). Tritiated S-methyl-DM1 bound to 37 high-affinity sites per microtubule (Kd of 0.1 μM)[1].
The concentration dependence curves for the inhibition of cell proliferation by S-methyl DM1 is sigmoidal in shape in MCF7 cells. Minimal inhibition occurred at 200 pM S-methyl DM1, and inhibition is maximal at 3 nM. S-methyl DM1 (IC50 of 330 pM) is slightly more potent than Maytansine (IC50 of 710 pM)[2].
S-methyl DM1 induces maxima of 80% accumulation of cells in G2/M as compared with only 30% in controls in MCF7 cells[2].

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

Molecular Weight

752.31

Formula

C36H50ClN3O10S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@]1([C@@](CC(N(C2=CC3=CC(OC)=C2Cl)C)=O)([H])OC([C@H](C)N(C)C(CCSC)=O)=O)[C@H]([C@@H]([C@](OC4=O)([H])C[C@]([C@](/C=C/C=C(C)/C3)([H])OC)(N4)O)C)O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (132.92 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 1.3292 mL 6.6462 mL 13.2924 mL
5 mM 0.2658 mL 1.3292 mL 2.6585 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.32 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:

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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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+
%
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3292 mL 6.6462 mL 13.2924 mL 33.2310 mL
5 mM 0.2658 mL 1.3292 mL 2.6585 mL 6.6462 mL
10 mM 0.1329 mL 0.6646 mL 1.3292 mL 3.3231 mL
15 mM 0.0886 mL 0.4431 mL 0.8862 mL 2.2154 mL
20 mM 0.0665 mL 0.3323 mL 0.6646 mL 1.6615 mL
25 mM 0.0532 mL 0.2658 mL 0.5317 mL 1.3292 mL
30 mM 0.0443 mL 0.2215 mL 0.4431 mL 1.1077 mL
40 mM 0.0332 mL 0.1662 mL 0.3323 mL 0.8308 mL
50 mM 0.0266 mL 0.1329 mL 0.2658 mL 0.6646 mL
60 mM 0.0222 mL 0.1108 mL 0.2215 mL 0.5538 mL
80 mM 0.0166 mL 0.0831 mL 0.1662 mL 0.4154 mL
100 mM 0.0133 mL 0.0665 mL 0.1329 mL 0.3323 mL
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S-methyl DM1
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HY-100504
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