2. Antibody-drug Conjugate/ADC Related Anti-infection Cytoskeleton Cell Cycle/DNA Damage
  3. ADC Cytotoxin Antibiotic Microtubule/Tubulin
  4. Tubulysin A

Tubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC50 values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin< b>ADC Cytotoxin.

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Tubulysin A Chemical Structure

Tubulysin A Chemical Structure

CAS No. : 205304-86-5

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Based on 1 publication(s) in Google Scholar

Tubulysin A Related Antibodies

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1 Publications Citing Use of MCE Tubulysin A

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Description

Tubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC50 values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin< b>ADC Cytotoxin[1][2][3][4].

IC50 & Target

Traditional Cytotoxic Agents

 

In Vitro

The IC50 values of Tubulysin A in the NCI-H1299 (lung), HT-29 (colon) and A2780 (ovary) cell lines are 3, 1 and 2 nmol/L, respectively[4].
The IC50 values of Tubulysin A against L929 (mouse fibroblast) and KB-V1 (human cervical cancer multidrug resistant cell line) cells were 0.07 and 1.4 ng/ml, respectively[1].
Tubulysin A (1 nM, 10 nM; 24h) has an antiangiogenic effect in HUVEC cells with IC50 values of 2.07-2.97 nM[1].
Tubulysin A (5h) can inhibit cell migration in HUVEC cells with IC50 value of 2.26 nM[1].
Tubulysin A (72h) can inhibit cell growth in HUVEC cells with GI50 value of 0.34 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tubulysin A Related Antibodies

Apoptosis Analysis[1]

Cell Line: HL-60 cells
Concentration: 0-100 nM
Incubation Time: 24/48h
Result: Had a strong pro-apoptotic effect on HL-60 tumor cell line, but had no significant effect on HUVEC cell line.

Cell Line:
Concentration:
Incubation Time:
Result:
In Vivo

Tubulysin A (0.04 mg/kg, 0.06 mg/kg; Intraperitoneal (i.p.); once daily for 4 days) can inhibit the growth of tumor cells in mouse xenotransplantation model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mouse xenotransplantation model[1]
Dosage: 0.04 and 0.06 mg/kg
Administration: Intraperitoneal (i.p.)
Result: Inhibited the growth of tumor cells.
Molecular Weight

844.07

Formula

C43H65N5O10S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C([C@@]([C@@H](C)CC)([H])NC([C@@H](CCCC1)N1C)=O)N(COC(CC(C)C)=O)[C@@H](C(C)C)C[C@H](C2=NC(C(N[C@H](C[C@H](C)C(O)=O)CC3=CC=C(O)C=C3)=O)=CS2)OC(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (118.47 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 1.1847 mL 5.9237 mL 11.8474 mL
5 mM 0.2369 mL 1.1847 mL 2.3695 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 (protect from light, stored under nitrogen). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (2.96 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 (2.96 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:

Dosage

mg/kg

Animal weight
(per animal)

g

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, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: 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 (protect from light, stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.08%

COA (251 KB) HNMR (408 KB) RP-HPLC (262 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

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 (protect from light, stored under nitrogen). 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 1.1847 mL 5.9237 mL 11.8474 mL 29.6184 mL
5 mM 0.2369 mL 1.1847 mL 2.3695 mL 5.9237 mL
10 mM 0.1185 mL 0.5924 mL 1.1847 mL 2.9618 mL
15 mM 0.0790 mL 0.3949 mL 0.7898 mL 1.9746 mL
20 mM 0.0592 mL 0.2962 mL 0.5924 mL 1.4809 mL
25 mM 0.0474 mL 0.2369 mL 0.4739 mL 1.1847 mL
30 mM 0.0395 mL 0.1975 mL 0.3949 mL 0.9873 mL
40 mM 0.0296 mL 0.1481 mL 0.2962 mL 0.7405 mL
50 mM 0.0237 mL 0.1185 mL 0.2369 mL 0.5924 mL
60 mM 0.0197 mL 0.0987 mL 0.1975 mL 0.4936 mL
80 mM 0.0148 mL 0.0740 mL 0.1481 mL 0.3702 mL
100 mM 0.0118 mL 0.0592 mL 0.1185 mL 0.2962 mL
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Tubulysin A Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tubulysin A205304-86-5TubAADC CytotoxinAntibioticMicrotubule/TubulinADC PayloadantiangiogenesismicrotubuleantiproliferativeHuman HT29 colorectalhuman A2780 ovarianhuman NCI-H1299 non-small cell lung carcinoma cells.Inhibitorinhibitorinhibit

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