Tubulin polymerization-IN-89

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Tubulin polymerization-IN-89 is a tubulin polymerization inhibitor. Tubulin polymerization-IN-89 binds to the colchicine-binding site on tubulin heterodimers, disrupting tubulin polymerization and microtubule formation. Tubulin polymerization-IN-89 induces apoptosis in melanoma cells and arrests the cell cycle at the G₂/M phase. Tubulin polymerization-IN-89 can be used in studies related to metastatic melanoma.

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Tubulin polymerization-IN-89 Estructura química

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Descripciòn

In Vitro

Tubulin polymerization-IN-89 (compound 9d) (100 nM; 24 h) disrupts the microtubule network, induces G₂/M phase cell cycle arrest, and triggers apoptosis in A375 cells by activating cleaved caspase-3 and cleaved PARP^[1].
Tubulin polymerization-IN-89 exhibits potent cytotoxicity in various melanoma cell lines, with the following GI₅₀ values: A375 (15.4 nM), RPMI-7951 (17.0 nM), A2058 (13.8 nM), and the paclitaxel-resistant strain A375/TxR (24.7 nM)^[1].
Tubulin polymerization-IN-89 (20-40 nM; 24 h) inhibits migration and invasion of A375/TxR cells^[1].
Tubulin polymerization-IN-89 (25-100 nM) completely abolishes colony formation in A375 cells^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	A375 melanoma cells
Concentration:	100 nM
Incubation Time:	24 h
Result:	Induced G2/M cell cycle arrest, with 80% of cells in G2/M phase.

Cell Migration Assay^[1]

Cell Line:	paclitaxel-resistant A375/TxR cells
Concentration:	20, 40 nM
Incubation Time:	24 h
Result:	Inhibited cell migration by 86% at 40 nM.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_last	AUC_inf	MRT_0-inf
Mice^[1]	10 mg/kg	i.p.	1.49 h	8.34 min	316 ng/mL	263 ng·h/mL	271 ng·h/mL	1.37 h

In Vivo

Tubulin polymerization-IN-89 (10-15 mg/kg; i.p.; three times per week; 17 days) exerts anti-tumor activity in a Paclitaxel (HY-B0015)-resistant melanoma xenograft mouse model^[1].

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

Animal Model:	NOD scid gamma (NSG) (female, 6−8 weeks old)^[1]
Dosage:	10 mg/kg; 15 mg/kg
Administration:	i.p.; 3x per week
Result:	Reduced mean ex vivo tumor volume and tumor weight. Decreased Ki67-positive area. Increased cleaved caspase-3-positive area. Increased CD45-positive area. Reduced viable tumor area.

Peso molecular

335.36

Fòrmula

C₁₈H₁₇N₅O₂

SMILES

CCNC1=NC2=CC=CC=C2N3C1=NN=C3C4=CC(O)=C(OC)C=C4

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Clark CJ, et al. Novel Triazoloquinoxaline-Based Tubulin Polymerization Inhibitor Induces Necroptosis and Significantly Inhibits Metastatic Melanoma Tumor Growth. J Med Chem. 2026;69(6):6461-6489. [Content Brief]