Tubulin inhibitor 11

Name: Tubulin inhibitor 11
Brand: MedChemExpress
SKU: HY-152156
Rating: 4.5 (1 reviews)

Cat. No.: HY-152156 Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

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Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis.

For research use only. We do not sell to patients.

Tubulin inhibitor 11 Chemical Structure

CAS No. : 2366260-33-3

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.025 μM Compound: 48	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
A549	IC₅₀	0.03 μM Compound: 48	Antiproliferative activity against paclitaxel-resistant human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against paclitaxel-resistant human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
B16-F10	IC₅₀	0.002 μM Compound: 48	Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
BGC-823	IC₅₀	0.021 μM Compound: 48	Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
DU-145	IC₅₀	0.004 μM Compound: 48	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 96 hrs by real-time cell analysis Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 96 hrs by real-time cell analysis	[PMID: 36511661]
DU-145	IC₅₀	0.008 μM Compound: 48	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
DU-145	IC₅₀	0.009 μM Compound: 48	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by real-time cell analysis Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by real-time cell analysis	[PMID: 36511661]
DU-145	IC₅₀	0.01 μM Compound: 48	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 24 hrs by real-time cell analysis Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 24 hrs by real-time cell analysis	[PMID: 36511661]
DU-145	IC₅₀	0.01 μM Compound: 48	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by real-time cell analysis Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by real-time cell analysis	[PMID: 36511661]
HCT-116	IC₅₀	0.004 μM Compound: 48	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
HCT-8	IC₅₀	0.022 μM Compound: 48	Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
HepG2	IC₅₀	0.003 μM Compound: 48	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
HGC-27	IC₅₀	0.006 μM Compound: 48	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
HUVEC	IC₅₀	0.032 μM Compound: 48	Anti-angiogenesis activity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Anti-angiogenesis activity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
MCF7	IC₅₀	0.006 μM Compound: 48	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
MCF7R	IC₅₀	0.014 μM Compound: 48	Antiproliferative activity against paclitaxel-resistant human MCF7R cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against paclitaxel-resistant human MCF7R cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
MDA-MB-231	IC₅₀	0.009 μM Compound: 48	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
NCI-H1299	IC₅₀	0.004 μM Compound: 48	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
NCI-H1437	IC₅₀	0.002 μM Compound: 48	Antiproliferative activity against human NCI-H1437 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1437 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
NCI-H460	IC₅₀	0.077 μM Compound: 48	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
SW1990	IC₅₀	0.015 μM Compound: 48	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 36511661]
Vero	IC₅₀	0.04 μM Compound: 48	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs	[PMID: 36511661]

In Vitro

Tubulin inhibitor 11 (Compound 48; 0.03-0.1 μM; 12 hours) causes cell cycle arrest at G2/M phase. Tubulin inhibitor 11 reduces cdc2 phosphorylation and increases cyclin B1 and phosphorylation of histone H3 at Ser10 in cells^[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM; 48 hours) causes cancer cell apoptosis^[1].
Tubulin inhibitor 11 (Compound 48) demonstrates favorable antiproliferative activities in DU145 cells with an IC₅₀ of 8 nM^[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM) significantly reduces the expression levels of acetyl-α-tubulin and α-tubulin in a dose-dependent manner^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	DU145 cells
Concentration:	0.01 μM, 0.03 μM, and 0.1 μM
Incubation Time:	12 hours
Result:	Caused cell cycle arrest at G2/M phase.

Apoptosis Analysis^[1]

Cell Line:	DU145 cells
Concentration:	0.03 μM, 0.1 μM, and 0.3 μM
Incubation Time:	48 hours
Result:	Induced cancer cell apoptosis.

Western Blot Analysis^[1]

Cell Line:	DU145 cells
Concentration:	0.01 μM, 0.03 μM, and 0.1 μM
Incubation Time:	12 hours
Result:	Reduced cdc2 phosphorylation and increased cyclin B1 and phosphorylation of histone H3 at Ser10 in cells.

In Vivo

Tubulin inhibitor 11 (Compound 48; 5-10 mg/kg; p.o; once daily) shows robust in vivo antitumor efficacies^[1].

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

Animal Model:	Male athymic BALB/c nude mice (18-20 g) injected with DU145, NCI-H1299 or A549R cells^[1]
Dosage:	5 mg/kg, 10 mg/kg
Administration:	p.o; once daily
Result:	Effectively suppressed tumor growth.

Molecular Weight

409.50

Formula

C₂₂H₂₃N₃O₃S

CAS No.

2366260-33-3

Appearance

Solid

Color

Off-white to pink

SMILES

O=C(C1=CC=C(C(NS(C2=CC=C(C=C2)C)(=O)=O)=C1)C)NCC3=CN=C(C=C3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (244.20 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	2.4420 mL	12.2100 mL	24.4200 mL
5 mM	0.4884 mL	2.4420 mL	4.8840 mL
10 mM	0.2442 mL	1.2210 mL	2.4420 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 (6.11 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 (6.11 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 (6.11 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, . 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.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (245 KB) HNMR (274 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Songwen Lin, et al. Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. J Med Chem. 2022 Dec 22;65(24):16372-16391. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4420 mL	12.2100 mL	24.4200 mL	61.0501 mL
	5 mM	0.4884 mL	2.4420 mL	4.8840 mL	12.2100 mL
	10 mM	0.2442 mL	1.2210 mL	2.4420 mL	6.1050 mL
	15 mM	0.1628 mL	0.8140 mL	1.6280 mL	4.0700 mL
	20 mM	0.1221 mL	0.6105 mL	1.2210 mL	3.0525 mL
	25 mM	0.0977 mL	0.4884 mL	0.9768 mL	2.4420 mL
	30 mM	0.0814 mL	0.4070 mL	0.8140 mL	2.0350 mL
	40 mM	0.0611 mL	0.3053 mL	0.6105 mL	1.5263 mL
	50 mM	0.0488 mL	0.2442 mL	0.4884 mL	1.2210 mL
	60 mM	0.0407 mL	0.2035 mL	0.4070 mL	1.0175 mL
	80 mM	0.0305 mL	0.1526 mL	0.3053 mL	0.7631 mL
	100 mM	0.0244 mL	0.1221 mL	0.2442 mL	0.6105 mL