Rosabulin

• CAT Number: I009185
• CAS Number: 501948-05-6
• Molecular Formula: C22H16N4O2S
• Molecular Weight: 400.45
• Purity: ≥95%
• Synonyms: 2-[3-[(4-cyanophenyl)methyl]indolizin-1-yl]-N-(3-methyl-1,2-thiazol-5-yl)-2-oxoacetamide
• InChI: InChI=1S/C22H16N4O2S/c1-14-10-20(29-25-14)24-22(28)21(27)18-12-17(26-9-3-2-4-19(18)26)11-15-5-7-16(13-23)8-6-15/h2-10,12H,11H2,1H3,(H,24,28)
• InChIKey: IZZYUABKZYIINT-UHFFFAOYSA-N
• SMILES: CC1=NSC(=C1)NC(=O)C(=O)C2=C3C=CC=CN3C(=C2)CC4=CC=C(C=C4)C#N

Rosabulin (STA 5312) is a potent and orally active microtubule inhibitor that inhibits microtubule assembly. Rosabulin has broad-spectrum anti-tumor activity[1].
Rosabulin (STA 5312) demonstrates substantial anti-proliferative activity against a wide range of cancer cell linesin vitro, including hematologic and solid tumor cell lines of various origins (e.g. leukemia, lymphoma, breast, colon, uterine), with IC50 values extending down into the nanomolar range. Cell lines with multi-drug resistant (MDR) phenotypes are similarly sensitive to Rosabulin. The mechanism of action for Rosabulin is inhibition of microtubule assembly and subsequent arrest of the cell cycle[1].
When dosed orally or intravenously, Rosabulin (STA 5312) has shown in vivo activity in several murine tumors as well as human tumor xenograft models, including drug resistant tumors[1].

Reference

[1]. Keizo Koya,et al. STA-5312, a novel tubulin inhibitor, demonstrates the anti-cancer activity against chemotherapy-resistant cancers. Cancer Res, Volume 45, 2004.