2. Antibody-drug Conjugate/ADC Related Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. ADC Payload Microtubule/Tubulin Apoptosis
  4. Tubulysin

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Tubulysin

Tubulysin 構造式

CAS 番号 : 1943604-24-7

容量 価格（税別） 在庫状況 数量
1 mg $960 在庫あり
5 mg $2400 在庫あり
10 mg   お問い合わせ  
50 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Tubulysin 関連抗体

Top Publications Citing Use of Products

ADC Payload アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Auristatin Calicheamicins Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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[1][2][3].

Cellular Effect
Cell Line Type Value Description References
786-0 EC50
0.57 nM
Compound: Tubulysin
Antiproliferative activity in human 786-0 cells
Antiproliferative activity in human 786-0 cells
[PMID: 38097140]
LNCaP IC50
2.5 nM
Compound: Tub
Cytotoxicity against human LNCAP cells
Cytotoxicity against human LNCAP cells
[PMID: 20936874]
体外実験

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.

Tubulysin 関連抗体
分子量

842.10

分子式

C44H67N5O9S
CAS 番号
Appearance

Solid

Color

White to off-white

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1875 mL 5.9375 mL 11.8751 mL
5 mM 0.2375 mL 1.1875 mL 2.3750 mL
10 mM 0.1188 mL 0.5938 mL 1.1875 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 (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.

  • 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)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (2.97 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.
  • Protocol 2

    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:

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 (stored under nitrogen, away from moisture)

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.
純度とドキュメンテーション
参考文献

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
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Tubulysin Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

Tubulysin1943604-24-7ADC PayloadMicrotubule/TubulinApoptosisADC CytotoxinCYP1A2Vinca alkaloid binding sitenude micetubulin polymerizationβ-tubulinprostate cancerCYP2D6CYP3A4apoptosishuman cancer cellsInhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
Tubulysin
製品番号:
HY-128914
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.