Tubulysin M
Based on 1 Customer Validation
Tubulysin M is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin M can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin M displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin M inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis.
For research use only. We do not sell to patients.
- Purity: 98.74%
- CAS No.: 936691-46-2
- Formula: C38H57N5O7S
- Molecular Weight:727.95
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | GI50 |
0.71 nM
Compound: 1
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Cytotoxicity against human DU145 cells incubated for 72 hrs by alamar blue abased assay
Cytotoxicity against human DU145 cells incubated for 72 hrs by alamar blue abased assay
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[PMID: 27809515] |
| HCT-116 | GI50 |
0.62 nM
Compound: 1
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Cytotoxicity against human HCT116 cells incubated for 72 hrs by alamar blue abased assay
Cytotoxicity against human HCT116 cells incubated for 72 hrs by alamar blue abased assay
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[PMID: 27809515] |
| KB | IC50 |
0.33 nM
Compound: 1; N-14-desacetoxytubulysin H
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Cytotoxicity against MDR1 deficient human KB cells assessed as decrease in cell viability after 4 days by MTS assay
Cytotoxicity against MDR1 deficient human KB cells assessed as decrease in cell viability after 4 days by MTS assay
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[PMID: 27882198] |
| KB 3-1 | IC50 |
0.19 nM
Compound: 1
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Cytotoxicity against human KB-3-1 cells
Cytotoxicity against human KB-3-1 cells
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[PMID: 27809515] |
| L-428 | EC50 |
0.04 nM
Compound: 2; TubM
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Antiproliferative against human L428 cells incubated for 96 hrs by cellTiter-Glo assay
Antiproliferative against human L428 cells incubated for 96 hrs by cellTiter-Glo assay
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[PMID: 32527543] |
| L-540 | EC50 |
0.08 nM
Compound: 2; TubM
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Antiproliferative against human L540cy cells incubated for 96 hrs by cellTiter-Glo assay
Antiproliferative against human L540cy cells incubated for 96 hrs by cellTiter-Glo assay
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[PMID: 32527543] |
| L929 | IC50 |
0.34 nM
Compound: 1
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Cytotoxicity against mouse L929 cells
Cytotoxicity against mouse L929 cells
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[PMID: 27809515] |
| MDA-MB-231 | GI50 |
1.14 nM
Compound: 1
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Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by alamar blue abased assay
Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by alamar blue abased assay
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[PMID: 27809515] |
| MDA-MB-361 | IC50 |
0.13 nM
Compound: 1; N-14-desacetoxytubulysin H
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Cytotoxicity against human MDA-MB-361/DYT2 cells assessed as decrease in cell viability after 4 days by MTS assay
Cytotoxicity against human MDA-MB-361/DYT2 cells assessed as decrease in cell viability after 4 days by MTS assay
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[PMID: 27882198] |
| NCI-N87 | IC50 |
0.46 nM
Compound: 1; N-14-desacetoxytubulysin H
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Cytotoxicity against human NCI-N87 cells assessed as decrease in cell viability after 4 days by MTS assay
Cytotoxicity against human NCI-N87 cells assessed as decrease in cell viability after 4 days by MTS assay
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[PMID: 27882198] |
| SW480 | IC50 |
0.02 nM
Compound: 1
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Cytotoxicity against human SW480 cells
Cytotoxicity against human SW480 cells
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[PMID: 27809515] |
| T98 | IC50 |
1.6 nM
Compound: 1
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Cytotoxicity against human T98 cells
Cytotoxicity against human T98 cells
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[PMID: 27809515] |
Tubulysin M binds to both the vinca domain and the tubulin β2 subunit alone, forms additional interactions with tubulin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 936691-46-2
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Appearance Solid
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Molecular Weight 727.95
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Formula C38H57N5O7S
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Color White to light yellow
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SMILES
O=C(N[C@@H]([C@@H](C)CC)C(N(C)[C@@H](C(C)C)C[C@@H](OC(C)=O)C1=NC(C(N[C@@H](CC2=CC=CC=C2)C[C@H](C)C(O)=O)=O)=CS1)=O)[C@@H]3N(C)CCCC3
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Structure Classification
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Initial Source
Archangium gephyra
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (137.37 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. 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. 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 (3.43 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 (3.43 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.
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 (273 KB)
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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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang Y, et al. Structural Insights into the Pharmacophore of Vinca Domain Inhibitors of Microtubules. Mol Pharmacol. 2016 Feb;89(2):233-42. [Content Brief]
[2]. Kubicek K, et al. The tubulin-bound structure of the antimitotic drug tubulysin. Angew Chem Int Ed Engl. 2010 Jun 28;49(28):4809-12. [Content Brief]
[3]. Vlahov IR, et al. Acid mediated formation of an N-acyliminium ion from tubulysins: a new methodology for the synthesis of natural tubulysins and their analogs. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6778-81. [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. 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 | 1.3737 mL | 6.8686 mL | 13.7372 mL | 34.3430 mL |
| 5 mM | 0.2747 mL | 1.3737 mL | 2.7474 mL | 6.8686 mL | |
| 10 mM | 0.1374 mL | 0.6869 mL | 1.3737 mL | 3.4343 mL | |
| 15 mM | 0.0916 mL | 0.4579 mL | 0.9158 mL | 2.2895 mL | |
| 20 mM | 0.0687 mL | 0.3434 mL | 0.6869 mL | 1.7172 mL | |
| 25 mM | 0.0549 mL | 0.2747 mL | 0.5495 mL | 1.3737 mL | |
| 30 mM | 0.0458 mL | 0.2290 mL | 0.4579 mL | 1.1448 mL | |
| 40 mM | 0.0343 mL | 0.1717 mL | 0.3434 mL | 0.8586 mL | |
| 50 mM | 0.0275 mL | 0.1374 mL | 0.2747 mL | 0.6869 mL | |
| 60 mM | 0.0229 mL | 0.1145 mL | 0.2290 mL | 0.5724 mL | |
| 80 mM | 0.0172 mL | 0.0859 mL | 0.1717 mL | 0.4293 mL | |
| 100 mM | 0.0137 mL | 0.0687 mL | 0.1374 mL | 0.3434 mL |
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