Tubulin polymerization-IN-65

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Tubulin polymerization-IN-65 is a tubulin polymerisation inhibitor with a broad spectrum cytotoxic. Tubulin polymerization-IN-65 induces G2 + M cell cycle arrest.

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Tubulin polymerization-IN-65 Chemical Structure

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Purity & Documentation
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Description

Tubulin polymerization-IN-65 is a tubulin polymerisation inhibitor with a broad spectrum cytotoxic. Tubulin polymerization-IN-65 induces G2 + M cell cycle arrest^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	GI₅₀	0.33 μM Compound: 64	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 38784470]
A2780	GI₅₀	0.33 μM Compound: 64	Antiproliferative activity against human A2780 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 38784470]
A549	IC₅₀	> 25 μM Compound: 4	Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
BE(2)-C	GI₅₀	0.31 μM Compound: 64	Antiproliferative activity against human BE2C cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human BE2C cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 38784470]
DU-145	GI₅₀	0.9 μM Compound: 64	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 38784470]
HCT-116	IC₅₀	1.46 μM Compound: 4	Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
HCT-116	IC₅₀	1.58 μM Compound: 5b	Cytotoxicity against human HCT116 cells after 24 to 96 hrs by MTS assay Cytotoxicity against human HCT116 cells after 24 to 96 hrs by MTS assay	[PMID: 20303768]
HCT-116	IC₅₀	2.47 μM Compound: 4	Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
HT-29	GI₅₀	0.26 μM Compound: 64	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 38784470]
MCF-10A	GI₅₀	0.56 μM Compound: 64	Cytotoxicity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 38784470]
MCF7	GI₅₀	0.35 μM Compound: 64	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 38784470]
MCF7	IC₅₀	4.45 μM Compound: 4	Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
MIA PaCa-2	GI₅₀	0.37 μM Compound: 64	Antiproliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 38784470]
NCI-H460	GI₅₀	0.42 μM Compound: 64	Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 38784470]
NHDF	IC₅₀	> 25 μM Compound: 4	Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay	[PMID: 30562697]
NIH3T3	IC₅₀	1.17 μM Compound: 5b	Cytotoxicity against mouse NIH/3T3 cells assessed as viable cells after 72 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells assessed as viable cells after 72 hrs by MTT assay	[PMID: 20303768]
SK-N-MC	IC₅₀	2.88 μM Compound: 5b	Cytotoxicity against human SK-N-MC cells after 72 hrs by MTT assay Cytotoxicity against human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 20303768]
U-87MG ATCC	GI₅₀	1.4 μM Compound: 64	Antiproliferative activity against human U87 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human U87 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 38784470]

In Vitro

Tubulin polymerization-IN-65 (compound 64; 5 μM; 24 h) induces G2 + M cell cycle arrest^[1].
Tubulin polymerization-IN-65 (72 h) inhibits cell growth of HT29, U87, MC-7, A2780, H460, A431, Du145, BE2-C, SJ-G2, MIA, MCF10A,with GI₅₀ values of 0.26 μM,1.4 μM, 0.35 μM, 0.33 μM, 0.42 μM, 0.33 μM, 0.90 μM, 0.31 μM, 0.79 μM, 0.37 μM, and, 0.56 μM, respectively^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	MIA pancreatic cancer cells
Concentration:	5 μM
Incubation Time:	24 h
Result:	Induced G2 + M cell cycle arrest.

Molecular Weight

278.31

Formula

C₁₇H₁₄N₂O₂

SMILES

O=C1NC(/C=C/C2=CC=CC=C2OC)=NC3=CC=CC=C31

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]. Nicholas S O'Brien, et al. 2,3-Dihydroquinazolin-4(1 H)-ones and quinazolin-4(3 H)-ones as broad-spectrum cytotoxic agents and their impact on tubulin polymerisation. RSC Med Chem. 2024 Mar 6;15(5):1686-1708. [Content Brief]