| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Tubulysin M targets tubulin, the protein that polymerizes to form microtubules. By inhibiting tubulin polymerization, it disrupts the mitotic spindle, leading to cell cycle arrest at the G2/M phase and subsequent apoptosis. It displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with U₅₀ values in the lower nanomolar range.
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|---|---|
| ln Vitro |
In vitro, Tubulysin M exhibits potent cytotoxic activity against various cancer cell lines, including multidrug-resistant cells, with U₅₀ values in the lower nanomolar range. It inhibits tubulin polymerization and induces depolymerization of isolated microtubules. The compound arrests cells in the G2/M phase of the cell cycle and induces apoptosis.
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| ln Vivo |
In vivo activity data for Tubulysin M are limited, as it is primarily used as the cytotoxic payload in antibody-drug conjugates (ADCs). When conjugated to a targeting antibody, it delivers potent cytotoxicity specifically to tumor cells. This approach enhances efficacy while reducing systemic toxicity. Further in vivo studies are needed to characterize its ADC applications.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Tubulysin M are performed using purified tubulin. The compound's ability to inhibit tubulin polymerization is measured spectrophotometrically by monitoring the increase in turbidity associated with microtubule formation. Depolymerization of pre-formed microtubules is also assessed. The IC₅₀ or U₅₀ values are calculated from concentration-response curves.
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| Cell Assay |
In vitro cellular assays for Tubulysin M are performed using cancer cell lines, including multidrug-resistant lines. Cells are treated with the compound at various concentrations (typically nM range) for 48-72 hours, and cell viability is assessed using MTT, CCK-8, or other cytotoxicity assays. Cell cycle analysis is performed by flow cytometry to measure G2/M arrest. Apoptosis is evaluated by annexin V staining or caspase activity assays.
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| Animal Protocol |
In vivo animal experiments for Tubulysin M are typically conducted as part of ADC development. The compound is conjugated to a targeting antibody and administered to mouse xenograft models bearing tumors expressing the target antigen. Efficacy is assessed by measuring tumor volume reduction, and toxicity is monitored by body weight and organ histology.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tubulysin M have not been fully characterized. The compound has a molecular weight of 727.95 and molecular formula C₃₈H₅₇N₅O₇S. It is supplied with purity ≥95%. The compound is used as the cytotoxic component in ADCs. Further PK studies are needed to determine its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicological data for Tubulysin M are not extensively reported. As a highly cytotoxic compound, it is expected to have significant toxicity if administered systemically. This is why it is typically used as a payload in ADCs to achieve targeted delivery to tumor cells. The compound is intended for research purposes only and is not approved for human therapeutic use.
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| References |
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| Additional Infomation |
Tubulysin M is a highly cytotoxic tubulysin D analog with CAS number 936691-46-2, molecular formula C₃₈H₅₇N₅O₇S, and molecular weight 727.95. It inhibits tubulin polymerization, arrests cells in G2/M, and induces apoptosis. It is used as the cytotoxic payload in antibody-drug conjugates (ADCs). This product is for research use only.
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| Molecular Formula |
C38H57N5O7S
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|---|---|
| Molecular Weight |
727.95348906517
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| Exact Mass |
727.397
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| CAS # |
936691-46-2
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| PubChem CID |
23634457
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
904.9±65.0 °C at 760 mmHg
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| Flash Point |
501.1±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.551
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| Source |
Originated from microorganisms: Archangium gephyra
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| LogP |
5.05
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
51
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| Complexity |
1170
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N(C)[C@H](C[C@H](C1=NC(=CS1)C(=O)N[C@@H](CC2=CC=CC=C2)C[C@H](C)C(=O)O)OC(=O)C)C(C)C)NC(=O)[C@H]3CCCCN3C
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| InChi Key |
POBZYODNVHQLFG-ZRBKHQLFSA-N
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| InChi Code |
InChI=1S/C38H57N5O7S/c1-9-24(4)33(41-35(46)30-17-13-14-18-42(30)7)37(47)43(8)31(23(2)3)21-32(50-26(6)44)36-40-29(22-51-36)34(45)39-28(19-25(5)38(48)49)20-27-15-11-10-12-16-27/h10-12,15-16,22-25,28,30-33H,9,13-14,17-21H2,1-8H3,(H,39,45)(H,41,46)(H,48,49)/t24-,25-,28+,30+,31+,32+,33-/m0/s1
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| Chemical Name |
(2S,4R)-4-[[2-[(1R,3R)-1-acetyloxy-4-methyl-3-[methyl-[(2S,3S)-3-methyl-2-[[(2R)-1-methylpiperidine-2-carbonyl]amino]pentanoyl]amino]pentyl]-1,3-thiazole-4-carbonyl]amino]-2-methyl-5-phenylpentanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~137.4 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (3.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3737 mL | 6.8686 mL | 13.7372 mL | |
| 5 mM | 0.2747 mL | 1.3737 mL | 2.7474 mL | |
| 10 mM | 0.1374 mL | 0.6869 mL | 1.3737 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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