Tubulysin
Based on 1 Customer Validation
Tubulysin is a microtubule destabilizer that binds to the β-tubulin peptide site adjacent to the vinca alkaloid binding site and inhibits tubulin polymerization. Tubulysin induces apoptosis and exhibits antiproliferative activity against a variety of human cancer cells, including multidrug-resistant strains. Tubulysin can be conjugated to antibodies via a disulfide-containing quaternary ammonium linker for ADC synthesis. Tubulysin is applicable to tumor-related research.
For research use only. We do not sell to patients.
- Purity : 99.60%
- CAS No.: 1943604-24-7
- Formula: C44H67N5O9S
- Molecular Weight:842.10
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Storage:
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, 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]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| 786-0 | EC50 |
0.57 nM
Compound: Tubulysin
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Antiproliferative activity in human 786-0 cells
Antiproliferative activity in human 786-0 cells
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[PMID: 38097140] |
| LNCaP | IC50 |
2.5 nM
Compound: Tub
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Cytotoxicity against human LNCAP cells
Cytotoxicity against human LNCAP cells
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[PMID: 20936874] |
In Vitro
Tubulysin is commonly utilized as a representative scaffold or tool compound in mechanistic studies and the development of Antibody-Drug Conjugates (ADCs). An Antibody-Drug Conjugate (ADC) is a novel therapeutic modality consisting of a humanized or fully human monoclonal antibody chemically linked to a highly cytotoxic small molecule (payload); it holds immense potential to drive a paradigm shift in cancer chemotherapy. This antibody-based molecular platform enables the selective delivery of potent cytotoxic payloads to targeted cancer cells, thereby enhancing therapeutic efficacy, reducing systemic toxicity, and achieving superior pharmacokinetics (PK), pharmacodynamics (PD), and biodistribution compared to traditional chemotherapy.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1943604-24-7
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Appearance Solid
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Molecular Weight 842.10
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Formula C44H67N5O9S
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Color White to off-white
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SMILES
O=C(O)[C@@H](C)C[C@@H](NC(C1=CSC([C@H](OC(C)=O)C[C@@H](N(COC(CC(C)C)=O)C([C@@H](NC([C@@H]2N(C)CCCC2)=O)[C@@H](C)CC)=O)C(C)C)=N1)=O)CC3=CC=C(C)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (118.75 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, 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 (stored under nitrogen, 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.97 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 (2.97 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:
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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, 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.
Protocols
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Leamon CP, et al. Prostate-Specific Membrane Antigen-Specific Antitumor Activity of a Self-Immolative Tubulysin Conjugate. Bioconjug Chem. 2019;30(6):1805-1813. [Content Brief]
[2]. Staben LR, et al. Targeted drug delivery through the traceless release of tertiary and heteroaryl amines from antibody-drug conjugates. Nat Chem. 2016;8(12):1112-1119. [Content Brief]
[3]. Murray BC, et al. Chemistry and biology of tubulysins: antimitotic tetrapeptides with activity against drug resistant cancers. Nat Prod Rep. 2015;32(5):654-662. [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, 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 |
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| DMSO | 1 mM | 1.1875 mL | 5.9375 mL | 11.8751 mL | 29.6877 mL |
| 5 mM | 0.2375 mL | 1.1875 mL | 2.3750 mL | 5.9375 mL | |
| 10 mM | 0.1188 mL | 0.5938 mL | 1.1875 mL | 2.9688 mL | |
| 15 mM | 0.0792 mL | 0.3958 mL | 0.7917 mL | 1.9792 mL | |
| 20 mM | 0.0594 mL | 0.2969 mL | 0.5938 mL | 1.4844 mL | |
| 25 mM | 0.0475 mL | 0.2375 mL | 0.4750 mL | 1.1875 mL | |
| 30 mM | 0.0396 mL | 0.1979 mL | 0.3958 mL | 0.9896 mL | |
| 40 mM | 0.0297 mL | 0.1484 mL | 0.2969 mL | 0.7422 mL | |
| 50 mM | 0.0238 mL | 0.1188 mL | 0.2375 mL | 0.5938 mL | |
| 60 mM | 0.0198 mL | 0.0990 mL | 0.1979 mL | 0.4948 mL | |
| 80 mM | 0.0148 mL | 0.0742 mL | 0.1484 mL | 0.3711 mL | |
| 100 mM | 0.0119 mL | 0.0594 mL | 0.1188 mL | 0.2969 mL |
Tubulysin Related Classifications
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