Referencia número: HY-116852

Thiocolchicine

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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 K_i of 0.7 µM. Thiocolchicine induces cell apoptosis. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.

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Pureza: 99.77%
No. CAS: 2730-71-4
Fòrmula: C₂₂H₂₅NO₅S
Peso molecular:415.50

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Thiocolchicine Chemical Structure

No. CAS: 2730-71-4

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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 K_i of 0.7 µM. Thiocolchicine induces cell apoptosis^[1]^[2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.5 μM Compound: 1	Cytotoxicity against human A549 cells after 24 hrs by MTS assay Cytotoxicity against human A549 cells after 24 hrs by MTS assay	[PMID: 19880222]
A549	ED₅₀	0.0019 μg/mL Compound: 2	Cytotoxicity against human A549 cells after 2 days Cytotoxicity against human A549 cells after 2 days	[PMID: 20542428]
A549	IC₅₀	0.6 μM Compound: Thiocolchicine	Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 27449957]
A549	IC₅₀	72 nM Compound: 6	Antiproliferative activity against human A549 cells incubated for 36 hrs Antiproliferative activity against human A549 cells incubated for 36 hrs	[PMID: 32432867]
A549	IC₅₀	11.3 nM Compound: 2	Antiproliferative activity against human A549 cells incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells incubated for 72 hrs by SRB assay	[PMID: 33465696]
A549	IC₅₀	0.9 nM Compound: TCOLCH	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay	[PMID: 34592435]
A549	ED₅₀	72 nM Compound: 3	Cytotoxicity against human solid tumor lung carcinoma A549 cell line Cytotoxicity against human solid tumor lung carcinoma A549 cell line	[PMID: 8496935]
BALB/3T3	IC₅₀	137 nM Compound: 2	Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs by SRB assay Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs by SRB assay	[PMID: 33465696]
BALB/3T3	IC₅₀	9.6 nM Compound: TCOLCH	Cytotoxicity against mouse BALB/3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against mouse BALB/3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 34592435]
CA46	IC₅₀	4.5 μM Compound: 2a	Inhibits the growth of the human Burkitt lymphoma CA46 cell Inhibits the growth of the human Burkitt lymphoma CA46 cell	[PMID: 9083485]
Caco-2	IC₅₀	0.5 μM Compound: 1	Cytotoxicity against human Caco-2 cells after 24 hrs by MTS assay Cytotoxicity against human Caco-2 cells after 24 hrs by MTS assay	[PMID: 19880222]
DLD-1	IC₅₀	4.2 nM Compound: Fig 15, Table R1C1	Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability	[PMID: 31655432]
DU-145	ED₅₀	0.0012 μg/mL Compound: 2	Cytotoxicity against human DU145 cells after 2 days Cytotoxicity against human DU145 cells after 2 days	[PMID: 20542428]
H9	EC₅₀	0.0018 μM Compound: 9	Cytotoxicity against human H9 cells Cytotoxicity against human H9 cells	[PMID: 1919593]
H9	IC₅₀	0.0017 μM Compound: 9	Antiviral activity against HIV1 HTLV-3B in human H9 cells after 3 days by p24 antigen capture assay Antiviral activity against HIV1 HTLV-3B in human H9 cells after 3 days by p24 antigen capture assay	[PMID: 1919593]
HCT-8	ED₅₀	0.008 μg/mL Compound: 2	Cytotoxicity against human HCT8 cells after 2 days Cytotoxicity against human HCT8 cells after 2 days	[PMID: 20542428]
HCT-8	IC₅₀	15 nM Compound: 6	Antiproliferative activity against human HCT-8 cells incubated for 36 hrs Antiproliferative activity against human HCT-8 cells incubated for 36 hrs	[PMID: 32432867]
HCT-8	ED₅₀	16 nM Compound: 3	Cytotoxicity against human solid tumor Colon carcinoma HCT-8 cell line Cytotoxicity against human solid tumor Colon carcinoma HCT-8 cell line	[PMID: 8496935]
HepG2	IC₅₀	0.5 μM Compound: 1	Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay	[PMID: 19880222]
IGROV-1	IC₅₀	0.012 μM Compound: 1	Antiproliferative activity against human IGROV1 cells assessed as growth inhibition after 72 hrs by Coulter counting analysis Antiproliferative activity against human IGROV1 cells assessed as growth inhibition after 72 hrs by Coulter counting analysis	[PMID: 19833515]
KB	ED₅₀	0.0008 μg/mL Compound: 2	Cytotoxicity against human KB cells after 2 days Cytotoxicity against human KB cells after 2 days	[PMID: 20542428]
KB	ED₅₀	0.8 ng/mL Compound: 2	Cytotoxicity against human KB cells after 2 days Cytotoxicity against human KB cells after 2 days	[PMID: 20542428]
KB	IC₅₀	0.04 nM Compound: 6	Antiproliferative activity against human KB cells incubated for 36 hrs Antiproliferative activity against human KB cells incubated for 36 hrs	[PMID: 32432867]
KB	ED₅₀	0.04 nM Compound: 3	Cytotoxicity against human solid tumor nasopharyngeal carcinoma KB cell line Cytotoxicity against human solid tumor nasopharyngeal carcinoma KB cell line	[PMID: 8496935]
L1210	IC₅₀	8 nM Compound: 6 (Thiocolchicine)	In vitro cytotoxicity against L1210 (murine leukemia) cells. In vitro cytotoxicity against L1210 (murine leukemia) cells.	[PMID: 2299625]
LoVo	IC₅₀	13.6 nM Compound: Fig 15, Table R1C1	Antiproliferative activity against human LoVo cells assessed as reduction in cell viability Antiproliferative activity against human LoVo cells assessed as reduction in cell viability	[PMID: 31655432]
LoVo	IC₅₀	21 nM Compound: 2	Antiproliferative activity against human LoVo cells incubated for 72 hrs by SRB assay Antiproliferative activity against human LoVo cells incubated for 72 hrs by SRB assay	[PMID: 33465696]
LoVo	IC₅₀	1 nM Compound: TCOLCH	Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay	[PMID: 34592435]
MCF7	IC₅₀	400 nM Compound: 2	Anti tumor activity on human breast cancer cell line MDR-positive MCF-7 ADRr after 72 hours of treatment Anti tumor activity on human breast cancer cell line MDR-positive MCF-7 ADRr after 72 hours of treatment	[PMID: 10602712]
MCF7	IC₅₀	0.1 μM Compound: Thiocolchicine	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 27449957]
MCF7	IC₅₀	55.5 nM Compound: Fig 15, Table R1C1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability	[PMID: 31655432]
MCF7	IC₅₀	9.6 nM Compound: 2	Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by SRB assay	[PMID: 33465696]
MCF7	IC₅₀	1.1 nM Compound: TCOLCH	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay	[PMID: 34592435]
MDA-MB-231	IC₅₀	0.6 nM Compound: 2	Anti tumor activity on human breast cancer cell line MDR-negative MDA-MB 231 after 72 hours of treatment Anti tumor activity on human breast cancer cell line MDR-negative MDA-MB 231 after 72 hours of treatment	[PMID: 10602712]
MDA-MB-231	IC₅₀	0.1 μM Compound: Thiocolchicine	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 27449957]
MDA-MB-231	IC₅₀	81.2 nM Compound: Fig 15, Table R1C1	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability	[PMID: 31655432]
MDA-MB-468	IC₅₀	0.2 μM Compound: Thiocolchicine	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 27449957]
P388	IC₅₀	5 nM Compound: 6	Antiproliferative activity against mouse P388 cells incubated for 36 hrs Antiproliferative activity against mouse P388 cells incubated for 36 hrs	[PMID: 32432867]
P388	ED₅₀	5 nM Compound: 3	Cytotoxicity against murine P388 leukemia cell line Cytotoxicity against murine P388 leukemia cell line	[PMID: 8496935]
RPMI-7951	IC₅₀	0.024 nM Compound: 6	Antiproliferative activity against human RPMI-7951 cells incubated for 36 hrs Antiproliferative activity against human RPMI-7951 cells incubated for 36 hrs	[PMID: 32432867]
RPMI-7951	ED₅₀	0.024 nM Compound: 3	Cytotoxicity against human melanoma RPMI-7951 cell line Cytotoxicity against human melanoma RPMI-7951 cell line	[PMID: 8496935]
SK-BR-3	ED₅₀	0.0015 μg/mL Compound: 2	Cytotoxicity against human SKBR3 cells after 2 days Cytotoxicity against human SKBR3 cells after 2 days	[PMID: 20542428]
T47D	IC₅₀	4.1 μM Compound: Thiocolchicine	Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 27449957]
TE-671	IC₅₀	0.024 nM Compound: 6	Antiproliferative activity against human TE-671 cells incubated for 36 hrs Antiproliferative activity against human TE-671 cells incubated for 36 hrs	[PMID: 32432867]
TE-671	ED₅₀	0.024 nM Compound: 3	Cytotoxicity against human central nervous system carcinoma TE671 cell line Cytotoxicity against human central nervous system carcinoma TE671 cell line	[PMID: 8496935]

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.

Chemical Information

No. CAS 2730-71-4
Appearance Solid
Peso molecular 415.50
Fòrmula C₂₂H₂₅NO₅S
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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4067 mL

12.0337 mL

24.0674 mL

5 mM

0.4813 mL

2.4067 mL

4.8135 mL

10 mM

0.2407 mL

1.2034 mL

2.4067 mL

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 KB)
SDS (251 KB)
- English - EN (251 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Thiocolchicine

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Thiocolchicine Related Classifications

HY-116852 Related Classifications