Tubulin inhibitor 1

Name: Tubulin inhibitor 1
Brand: MedChemExpress
SKU: HY-112607
Rating: 4.5 (1 reviews)

Cat. No.: HY-112607 Purity: 99.81%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.

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

Tubulin inhibitor 1 Chemical Structure

CAS No. : 2237054-53-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 88	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 88	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 128	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 256	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 410	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 660	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Tubulin^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	67 nM Compound: 7a3	Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay	[PMID: 30006162]
CT26	IC₅₀	58 nM Compound: 7a3	Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK8 assay Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK8 assay	[PMID: 30006162]
HeLa	IC₅₀	32.8 nM Compound: 7a3	Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay	[PMID: 30006162]
MCF7	IC₅₀	35.4 nM Compound: 7a3	Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay	[PMID: 30006162]
MDA-MB-231	IC₅₀	0.031 μM Compound: 7a3	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CCK8 assay	[PMID: 30006162]
SK-OV-3	IC₅₀	0.017 μM Compound: 7a3	Antiproliferative activity against human SKOV3 cells after 72 hrs by CCK8 assay Antiproliferative activity against human SKOV3 cells after 72 hrs by CCK8 assay	[PMID: 30006162]

In Vitro

Tubulin inhibitor 1 (Compound 7a3) is a tubulin inhibitor, inhibits tubulin polymerization^[1].
Tubulin inhibitor 1 has potent anti-proliferative activity against SK-OV-3, MDA-MB-231, HeLa, A549, CT26 and MCF-7 cells, with IC₅₀s of 16.7 ± 3.0, 31.4 ± 0.7, 32.8 ± 2.9, 67.0 ± 0.8, 58.0 ± 2.4 and 35.4 ± 5.6 nM, respectively^[1].
Tubulin inhibitor 1 (40, 80, and 160 nM, 48 hours) markedly causes cellular mitotic arrest in the G2/M phase, induces apoptosis in SK-OV-3 cells^[1].

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

Apoptosis Analysis^[1]

Cell Line:	SK-OV-3 cells
Concentration:	40, 80, and 160 nM
Incubation Time:	48 h
Result:	Induced apoptosis in SK-OV-3 cells after treatment for 48 h.

In Vivo

Tubulin inhibitor 1 (50 mg/kg, i.p., every two days three times for 20-25 days) is well tolerated, significantly reduces tumour growth in Balb/c nude mice bearing SK-OV-3 cells^[1].

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

Animal Model:	Six-week-old Balb/c nude mice (18-20 g) beraring SK-OV-3 cells^[1]
Dosage:	50 mg/kg
Administration:	I.P., every two days three times for 20-25 days
Result:	Significantly reduced tumour growth in Balb/c nude mice bearing SK-OV-3 cells, without obvious body weight loss.

Molecular Weight

368.43

Formula

C₂₁H₂₄N₂O₄

CAS No.

2237054-53-2

Appearance

Solid

Color

White to off-white

SMILES

CCOC1=CC=C(C2=CN(C)N=C2C3=CC(OC)=C(OC)C(OC)=C3)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 125 mg/mL (339.28 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7142 mL	13.5711 mL	27.1422 mL
5 mM	0.5428 mL	2.7142 mL	5.4284 mL
10 mM	0.2714 mL	1.3571 mL	2.7142 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.08 mg/mL (5.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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: 99.81%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (256 KB) HNMR (168 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

References

[1]. Lai Q, et al. Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3. Eur J Med Chem. 2018 Aug 5;156:162-179. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.7142 mL	13.5711 mL	27.1422 mL	67.8555 mL
	5 mM	0.5428 mL	2.7142 mL	5.4284 mL	13.5711 mL
	10 mM	0.2714 mL	1.3571 mL	2.7142 mL	6.7855 mL
	15 mM	0.1809 mL	0.9047 mL	1.8095 mL	4.5237 mL
	20 mM	0.1357 mL	0.6786 mL	1.3571 mL	3.3928 mL
	25 mM	0.1086 mL	0.5428 mL	1.0857 mL	2.7142 mL
	30 mM	0.0905 mL	0.4524 mL	0.9047 mL	2.2618 mL
	40 mM	0.0679 mL	0.3393 mL	0.6786 mL	1.6964 mL
	50 mM	0.0543 mL	0.2714 mL	0.5428 mL	1.3571 mL
	60 mM	0.0452 mL	0.2262 mL	0.4524 mL	1.1309 mL
	80 mM	0.0339 mL	0.1696 mL	0.3393 mL	0.8482 mL
	100 mM	0.0271 mL	0.1357 mL	0.2714 mL	0.6786 mL