Microtubule inhibitor 4

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Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC₅₀s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization.

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Microtubule inhibitor 4 Chemical Structure

CAS No. : 2411962-64-4

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	3.2 nM Compound: 2	Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32278711]
HCT-116	IC₅₀	3.8 nM Compound: 6o	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 31759826]
HeLa	IC₅₀	8.4 nM Compound: 6o	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 31759826]
HepG2	IC₅₀	3 nM Compound: 6o	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 31759826]
HT-29	IC₅₀	2.1 nM Compound: 2	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32278711]
MCF7	IC₅₀	9 nM Compound: 6o	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 31759826]
NCI-H460	IC₅₀	4 nM Compound: 2	Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32278711]
NCI-H460	IC₅₀	4 nM Compound: 6o	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by SRB assay Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 31759826]

Molecular Weight

446.47

Formula

C₂₅H₂₃FN₄O₃

CAS No.

2411962-64-4

SMILES

CC(C)(C1=C(N=CN1)/C=C2NC(/C(NC\2=O)=C/C3=CC(OC4=CC=C(C=C4)F)=CC=C3)=O)C

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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]. Ding Z, et al. Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer. Bioorg Med Chem. 2020 May 15;28(10):115435. [Content Brief]