Tubulysin M

Name: Tubulysin M
Brand: MedChemExpress
SKU: HY-N7053
Rating: 4.5 (1 reviews)

Cat. No.: HY-N7053 Purity: 98.74%: Data Sheet
SDS

COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

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.

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Tubulysin M Chemical Structure

CAS No. : 936691-46-2

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	Get quote
50 mg	Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Tubulysin M:

Des-methyl-Tubulysin M Get quote

View All ADC Cytotoxin Isoform Specific Products:

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	GI₅₀	0.71 nM Compound: 1	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	[PMID: 27809515]
HCT-116	GI₅₀	0.62 nM Compound: 1	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	[PMID: 27809515]
KB	IC₅₀	0.33 nM Compound: 1; N-14-desacetoxytubulysin H	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	[PMID: 27882198]
L-428	EC₅₀	0.04 nM Compound: 2; TubM	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	[PMID: 32527543]
L-540	EC₅₀	0.08 nM Compound: 2; TubM	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	[PMID: 32527543]
MDA-MB-231	GI₅₀	1.14 nM Compound: 1	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	[PMID: 27809515]
MDA-MB-361	IC₅₀	0.13 nM Compound: 1; N-14-desacetoxytubulysin H	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	[PMID: 27882198]
NCI-N87	IC₅₀	0.46 nM Compound: 1; N-14-desacetoxytubulysin H	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	[PMID: 27882198]

Molecular Weight

727.95

Formula

C₃₈H₅₇N₅O₇S

CAS No.

936691-46-2

Appearance

Solid

Color

White to light yellow

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

Structure Classification

Ketones, Aldehydes, Acids

Initial Source

Microorganisms

Archangium gephyra

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Purity & Documentation

Purity: 98.74%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (250 KB) HNMR (444 KB) RP-HPLC (256 KB) LCMS (95 KB)

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

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

Tubulysin M Related Classifications

Keywords:

Tubulysin M936691-46-2ADC CytotoxinMicrotubule/TubulinADC PayloadInhibitorinhibitorinhibit

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Tubulysin M

Customer Review

Other Forms of Tubulysin M:

View All ADC Cytotoxin Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tubulysin M Related Classifications

Keywords:

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