Tubulin inhibitor 14

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Tubulin inhibitor 14 is a potent NQO2 (quinone oxidoreductase 2) inhibitor with an IC₅₀ of 1.0 μM. Tubulin inhibitor 14 also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule-destabilizing agent with potential tumor-selectivity and antiangiogenic and vascular disrupting features.

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Tubulin inhibitor 14 Chemical Structure

CAS No. : 2767446-34-2

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC₅₀: 1.0 μM (NQO2)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.27 μM Compound: 4	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay	[PMID: 35290041]
A549	IC₅₀	0.44 μM Compound: 4	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay	[PMID: 35290041]
HCT-116	IC₅₀	0.13 μM Compound: 4	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay	[PMID: 35290041]
HCT-116	IC₅₀	0.13 μM Compound: 4	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay	[PMID: 35290041]
HepG2	IC₅₀	0.86 μM Compound: 4	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay	[PMID: 35290041]
HepG2	IC₅₀	1.44 μM Compound: 4	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay	[PMID: 35290041]
MCF7	IC₅₀	0.41 μM Compound: 4	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay	[PMID: 35290041]
MCF7	IC₅₀	0.5 μM Compound: 4	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay	[PMID: 35290041]
MDA-MB-231	IC₅₀	0.07 μM Compound: 4	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay	[PMID: 35290041]
MDA-MB-231	IC₅₀	0.09 μM Compound: 4	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay	[PMID: 35290041]
SNU-423	IC₅₀	0.25 μM Compound: 4	Antiproliferative activity against human SNU-423 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay Antiproliferative activity against human SNU-423 cells assessed as inhibition of cell proliferation incubated for 96 hrs by Sulforhodamine B assay	[PMID: 35290041]
SNU-423	IC₅₀	0.36 μM Compound: 4	Antiproliferative activity against human SNU-423 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay Antiproliferative activity against human SNU-423 cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by 72 hrs of compound-free incubation by Sulforhodamine B assay	[PMID: 35290041]

In Vitro

Tubulin inhibitor 14 (compound 4) (0-20 μM, 96 h) inhibits cancer cells proliferation ^[1].
Tubulin inhibitor 14 (1-5 μM, 24 or 48 h) causes G2/M cell cycle arrest^[1].
Tubulin inhibitor 14 (0.5-1 μM, 24 h) induces SNU423 cell apoptosis^[1].
Tubulin inhibitor 14 (0.5-1 μM, 24 h) disrupts the cytoskeleton network in endothelial cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	MDA-MB-231, HepG2, SNU423, A549, HCT116
Concentration:	0 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM, and 20 μM
Incubation Time:	96 h
Result:	Inhibited cell proliferation with IC₅₀ values of 0.41 μM (MCF-7) , 0.07 μM (MDA-MB-231), 1.44 μM (HepG2), 0.25 μM (SNU423), 0.27 μM (A549), and 0.13 μM (HCT116).

Cell Cycle Analysis^[1]

Cell Line:	HepG2 cells
Concentration:	1, 2, 5 μM
Incubation Time:	24 h, 48 h
Result:	Caused G2/M cell cycle arrest.

Apoptosis Analysis^[1]

Cell Line:	SNU423 cells
Concentration:	0.5, 1 μM
Incubation Time:	24 h
Result:	Induced SNU423 cell apoptosis.

Immunofluorescence^[1]

Cell Line:	HUVECs
Concentration:	0.5, 1 μM
Incubation Time:	24 h
Result:	Disrupted the cytoskeleton network in endothelial cells.

Molecular Weight

257.23

Formula

C₁₅H₉F₂NO

CAS No.

2767446-34-2

SMILES

O=C1NC(C2=CC=CC(F)=C2)=CC3=C1C=CC(F)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Mai A. Elhemely, et al. SAR of Novel 3-Arylisoquinolinones: meta-Substitution on the Aryl Ring Dramatically Enhances Antiproliferative Activity through Binding to Microtubules. J Med Chem. 2022 Mar 24;65(6):4783-4797. [Content Brief]