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Thiocolchicine [2730-71-4]

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Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 μM) and competitively binds to tubulin with a Ki of 0.7 μM. Thiocolchicine induces cell apoptosis. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.

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Thiocolchicine Chemical Structure

Thiocolchicine Chemical Structure

CAS No. : 2730-71-4

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

Based on 1 publication(s) in Google Scholar

Other Forms of Thiocolchicine:

  • Thiocolchicine-d3 Obtenir un devis
Description

Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 μM) and competitively binds to tubulin with a Ki of 0.7 μM. Thiocolchicine induces cell apoptosis[1][2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.

In Vitro

Thiocolchicine is against MCF-7, LoVo, LoVo/DX, A-549 and BALB/3T3 cells with IC50 values of 0.01 μM, 0.021 μM, 0.398 μM, 0.011 μM and 0.114 μM, respectively[3].
Thiocolchicine (1 nM-100 μM; 24-72 hours) shows a relationship between cell cycle blocking activity and growth inhibition in breast cancer cells. It inhibits cell proliferation of MDA-MB-231 and multidrug resistant (MDR) MCF-7 ADRr breast cancer cells with IC50s of 0.6 nM and 400 nM, respectively, as well as MDR CEM-VBL leukemia cells (IC50=50 nM)[2].

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

Thiocolchicine Related Antibodies
Masse moléculaire

415.50

Formule

C22H25NO5S
CAS No.

2730-71-4
Appearance

Solid

Color

Light yellow to green yellow

SMILES

CC(N[C@H](C1=C2)CCC3=CC(OC)=C(OC)C(OC)=C3C1=CC=C(SC)C2=O)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (240.67 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 2.4067 mL 12.0337 mL 24.0674 mL
5 mM 0.4813 mL 2.4067 mL 4.8135 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.

  • Calculateur de molarité

  • Calculateur de dilution

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 (6.02 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 (6.02 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).
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.
Pureté et documentation
Références

  • [1]. Klaus M.Hahn, et al. Structural requirements for the binding of colchicine analogs to tubulin: the role of the C-10 substituent. Bioorganic & Medicinal Chemistry Letters.Volume 1, Issue 9, 1991, Pages 471-476

    [2]. R De Vincenzo, et al. Antiproliferative Activity of Colchicine Analogues on MDR-positive and MDR-negative Human Cancer Cell Lines. Anticancer Drug Des. 1998 Jan;13(1):19-33.  [Content Brief]

  • [1]. Klaus M.Hahn, et al. Structural requirements for the binding of colchicine analogs to tubulin: the role of the C-10 substituent. Bioorganic & Medicinal Chemistry Letters.Volume 1, Issue 9, 1991, Pages 471-476

    [2]. R De Vincenzo, et al. Antiproliferative Activity of Colchicine Analogues on MDR-positive and MDR-negative Human Cancer Cell Lines. Anticancer Drug Des. 1998 Jan;13(1):19-33.

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4067 mL 12.0337 mL 24.0674 mL 60.1685 mL
5 mM 0.4813 mL 2.4067 mL 4.8135 mL 12.0337 mL
10 mM 0.2407 mL 1.2034 mL 2.4067 mL 6.0168 mL
15 mM 0.1604 mL 0.8022 mL 1.6045 mL 4.0112 mL
20 mM 0.1203 mL 0.6017 mL 1.2034 mL 3.0084 mL
25 mM 0.0963 mL 0.4813 mL 0.9627 mL 2.4067 mL
30 mM 0.0802 mL 0.4011 mL 0.8022 mL 2.0056 mL
40 mM 0.0602 mL 0.3008 mL 0.6017 mL 1.5042 mL
50 mM 0.0481 mL 0.2407 mL 0.4813 mL 1.2034 mL
60 mM 0.0401 mL 0.2006 mL 0.4011 mL 1.0028 mL
80 mM 0.0301 mL 0.1504 mL 0.3008 mL 0.7521 mL
100 mM 0.0241 mL 0.1203 mL 0.2407 mL 0.6017 mL
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Thiocolchicine Related Classifications

  • Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  • Microtubule/Tubulin Apoptosis
Help & FAQs

Keywords:

Thiocolchicine2730-71-4Microtubule/TubulinApoptosisMCF-7LoVoLoVo/DXA-549BALB/3T3breastcancerleukemiaAnalogueMDR-positiveColchicineInhibitorinhibitorinhibit