Tubulin inhibitor 11

• CAT Number: I042279
• CAS Number: 2366260-33-3
• Molecular Formula: C22H23N3O3S
• Molecular Weight: 409.50
• Purity: ≥95%
• Synonyms: 4-methyl-3-[(4-methylphenyl)sulfonylamino]-N-[(6-methylpyridin-3-yl)methyl]benzamide
• InChI: InChI=1S/C22H23N3O3S/c1-15-4-10-20(11-5-15)29(27,28)25-21-12-19(9-6-16(21)2)22(26)24-14-18-8-7-17(3)23-13-18/h4-13,25H,14H2,1-3H3,(H,24,26)
• InChIKey: ZKRBQBKMMRYJKN-UHFFFAOYSA-N
• SMILES: CC1=CC=C(C=C1)S(=O)(=O)NC2=C(C=CC(=C2)C(=O)NCC3=CN=C(C=C3)C)C

Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.1 μM; 12 hours) causes cell cycle arrest at G2/M phase. Tubulin inhibitor 11 reduces cdc2 phosphorylation and increases cyclin B1 and phosphorylation of histone H3 at Ser10 in cells[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM; 48 hours) causes cancer cell apoptosis[1].
Tubulin inhibitor 11 (Compound 48) demonstrates favorable antiproliferative activities in DU145 cells with an IC50 of 8 nM[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM) significantly reduces the expression levels of acetyl-α-tubulin and α-tubulin in a dose-dependent manner[1].
Tubulin inhibitor 11 (Compound 48; 5-10 mg/kg; p.o; once daily) shows robust in vivo antitumor efficacies[1].

Reference

[1]. Songwen Lin, et al. Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. J Med Chem. 2022 Dec 22;65(24):16372-16391.
 [Content Brief]