S-methyl DM1
Based on 1 Customer Validation
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.57%
- CAS. Nr.: 912569-84-7
- Formel: C36H50ClN3O10S
- Molecular Weight:752.31
-
Speicherung:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Toxins for Antibody-Drug Conjugate Research Library
HY-L023
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Covalent Screening Library
HY-L036
-
Macrocyclic Compound Library
HY-L041
-
Cytoskeleton Compound Library
HY-L060
-
Anti-Lung Cancer Compound Library
HY-L075
-
Protein-protein Interaction Inhibitor Library
HY-L109
-
Heterocyclic Compound Library
HY-L138
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Covalent Screening Library Plus
HY-L036P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
High-Efficiency Gene Editing Compound Library
HY-L244
Alle ADC Payloads Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
|
Maytansinoids |
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.
Chemical Information
-
CAS. Nr. 912569-84-7
-
Appearance Solid
-
Molecular Weight 752.31
-
Formel C36H50ClN3O10S
-
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
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Please enter the basic information of animal 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
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)
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.
Reinheit & Dokumentation
-
Data Sheet (282 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Lopus M, et al. Maytansine and cellular metabolites of antibody-maytansinoid conjugates strongly suppress microtubule dynamics by binding to microtubules. Mol Cancer Ther. 2010 Oct;9(10):2689-99. [Content Brief]
[2]. Oroudjev E, et al. Maytansinoid-antibody conjugates induce mitotic arrest by suppressing microtubule dynamic instability. Mol Cancer Ther. 2010 Oct;9(10):2700-13. [Content Brief]
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 |
S-methyl DM1 Related Classifications
HY-100504 Related Classifications
Powered by Bioz