Lys-SMCC-DM1
Based on 1 publication(s) in Google Scholar
Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is a agent-linker conjugates for ADC that can inhibit tubulin polymerization. Lys-SMCC-DM1 is the active metabolite of T-DM1. T-DM1 is a HER2-targeting ADC with a tubulin polymerization inhibitor DM1. Lys-SMCC-DM1 can be used in the research of breast cancer.
For research use only. We do not sell to patients.
- Purity: 99.25%
- CAS No.: 1281816-04-3
- Formula: C53H75ClN6O15S
- Molecular Weight:1103.71
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Lys-SMCC-DM1
MoreAll Drug-Linker Conjugates for ADC Isoforms
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Biological Activity
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Maytansinoids |
Lys-SMCC-DM1 possess a low level of permeability[1].
Lys-SMCC-DM1 shows cytotoxicity in KPL-4 and MDA-MB-468 cells, with IC50 of 24.8 nM and 40.5 nM respectively[2].
Lys-SMCC-DM1 (200 μM) inhibits the SLC46A3-mediated uptake of estrone 3-sulfate in MDCKII/SLC46A3 dC cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1281816-04-3
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Appearance Solid
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Molecular Weight 1103.71
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Formula C53H75ClN6O15S
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Color White to off-white
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SMILES
C[C@]1([C@@](CC(N(C(C=C2C=C3OC)=C3Cl)C)=O)([H])OC([C@H](C)N(C)C(CCS[C@@H](CC4=O)C(N4C[C@@H]5CC[C@@H](C(NCCCC[C@H](N)C(O)=O)=O)CC5)=O)=O)=O)[C@H]([C@@H]([C@](OC6=O)([H])C[C@]([C@](/C=C/C=C(C)/C2)([H])OC)(N6)O)C)O1
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Synonyms
Lys-Nε-MCC-DM1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Anal Chim Acta
Quantifying payloads of antibody‒drug conjugates using a postcolumn infused-internal standard strategy with LC‒MS. [Abstract]2024 May 15:1303:342537. PMID: 38609272
Solvent & Solubility
DMSO : 100 mg/mL (90.60 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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.27 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.27 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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 (stored under nitrogen)
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Ogitani Y, et al. Bystander killing effect of DS-8201a, a novel anti-human epidermal growth factor receptor 2 antibody-drug conjugate, in tumors with human epidermal growth factor receptor 2 heterogeneity. Cancer Sci. 2016 Jul;107(7):1039-46. [Content Brief]
[2]. Tomabechi R, et al. Identification of 5-Carboxyfluorescein as a Probe Substrate of SLC46A3 and Its Application in a Fluorescence-Based In Vitro Assay Evaluating the Interaction with SLC46A3. Mol Pharm. 2022 Dec 2. [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 (stored under nitrogen). 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 | 0.9060 mL | 4.5302 mL | 9.0604 mL | 22.6509 mL |
| 5 mM | 0.1812 mL | 0.9060 mL | 1.8121 mL | 4.5302 mL | |
| 10 mM | 0.0906 mL | 0.4530 mL | 0.9060 mL | 2.2651 mL | |
| 15 mM | 0.0604 mL | 0.3020 mL | 0.6040 mL | 1.5101 mL | |
| 20 mM | 0.0453 mL | 0.2265 mL | 0.4530 mL | 1.1325 mL | |
| 25 mM | 0.0362 mL | 0.1812 mL | 0.3624 mL | 0.9060 mL | |
| 30 mM | 0.0302 mL | 0.1510 mL | 0.3020 mL | 0.7550 mL | |
| 40 mM | 0.0227 mL | 0.1133 mL | 0.2265 mL | 0.5663 mL | |
| 50 mM | 0.0181 mL | 0.0906 mL | 0.1812 mL | 0.4530 mL | |
| 60 mM | 0.0151 mL | 0.0755 mL | 0.1510 mL | 0.3775 mL | |
| 80 mM | 0.0113 mL | 0.0566 mL | 0.1133 mL | 0.2831 mL |
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