| 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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| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (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.
Products are for research use only; We do not sell to patients
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