Tubulin polymerization-IN-41

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Tubulin polymerization-IN-41 is a potent tubulin polymerization inhibitor with the IC₅₀ of 2.61 μM. Tubulin polymerization-IN-41 targets the Colchicine-binding site of tubulin. Tubulin polymerization-IN-41 has anticancer effects.

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Tubulin polymerization-IN-41 Chemical Structure

CAS No. : 2804026-81-9

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	8.7 nM Compound: C3	Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay	[PMID: 36471625]
HT-29	IC₅₀	8.3 nM Compound: C3	Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay	[PMID: 36471625]
K562	IC₅₀	6.3 nM Compound: C3	Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay	[PMID: 36471625]
MCF7	IC₅₀	9.2 nM Compound: C3	Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay	[PMID: 36471625]

In Vitro

Tubulin polymerization-IN-41 (compound C3) displays remarkable antiproliferative activities with IC₅₀ values of 6.3 nM, 9.2 nM, 8.3 nM, and 8.7 nM for K562, MCF-7, HT29, and HCT116 cells, respectively. Additionally, Tubulin polymerization-IN-41 shows marked activity against Paclitaxel-resistant MCF-7 cells and A549 cells^[1].
Tubulin polymerization-IN-41 (compound C3; 5-20 nM) downregulates the expression of acetyl-α-tubulin (Ac-α-tubulin) and upregulated the expression of detyrosinated-α-tubulin (DeY-α-tubulin) in a concentration-dependent manner^[1].
Tubulin polymerization-IN-41 (compound C3; 5-20 nM; 24 hours) could arrest cancer cells in the G2/M phase, and induces MCF-7 cells apoptosis in a concentration-dependent manner^[1].
Tubulin polymerization-IN-41 (compound C3; 5-20 nM; 24 hours) reduces Ser216 phosphorylation, resulting in cdc2 Tyr15 dephosphorylation and Thr161 phosphorylation, which ultimately leads to the activation of subsequent cdc2/cyclin B1 complex^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	MCF-7 cells
Concentration:	5 nM, 10 nM, 20 nM
Incubation Time:	24 h
Result:	Could arrest cancer cells in the G2/M phase.

Apoptosis Analysis^[1]

Cell Line:	MCF-7 cells
Concentration:	5 nM, 10 nM, 20 nM
Incubation Time:	24 h
Result:	Induced MCF-7 cells apoptosis.

Western Blot Analysis^[1]

Cell Line:	MCF-7 cells
Concentration:	5 nM, 10 nM, 20 nM
Incubation Time:	24 h
Result:	Induced cdc25c activation.

In Vivo

Tubulin polymerization-IN-41 (compound C3; 5-20 mg/kg; i.p; every two days; for 21 consecutive days) exhibits the significant potency of tumor growth inhibition in a dose dependence without weight loss in the drug-treated period^[1].

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

Animal Model:	Five-week-old female athymic nude mice injected with MCF-7 cells^[1]
Dosage:	5, 10, and 20 mg/kg
Administration:	Intraperitoneal injection; every two days; for 21 consecutive days
Result:	Exhibited the significant potency of tumor growth inhibition in a dose dependence without weight loss in the drug-treated period.

Molecular Weight

435.26

Formula

C₂₀H₁₆Cl₂N₂O₅

CAS No.

2804026-81-9

SMILES

O=C(N1[C@@H](C2=CC3=C(C=C2C[C@H]14)OCCO3)C5=CC(Cl)=C(C(Cl)=C5)OC)NC4=O

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]. Jiafu Leng, et al. Discovery of Novel N-Heterocyclic-Fused Deoxypodophyllotoxin Analogues as Tubulin Polymerization Inhibitors Targeting the Colchicine-Binding Site for Cancer Treatment. J Med Chem. 2022 Dec 22;65(24):16774-16800. [Content Brief]