For research use only. Not for therapeutic Use.
MLN0905 is a potent, orally active Polo-like kinase 1 (PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC50 value of 2 nM. MLN0905 can be used for the research of cancer[1][2].
MLN0905 (compound 12c) has inhibitory potency against PLK1 with an IC50 value of 2 nM[1].
MLN0905 exhibits potent activities for Cdc25C with an EC50 value of 33 nM[1].
MLN0905 shows inhibitory effects on HT29, HCT116, H460, and A375 cell lines with LD50 values of 22 nM, 56 nM, 89 nM and 34 nM, respectively[1].
MLN0905 (125 nM) shows strong mitotic arrest and monopolar spindle formation in HT-29 cells[1].
MLN0905 suppresses the growth of lymphoma cell lines with IC50 values ranging from 3 – 24 nM[2].
MLN0905 (p.o.; 50 mg/kg) shows a high sustained PD response in nude mice HT29 xenograft tumors[1].
MLN0905 (p.o.; 6.25, 12.5, 25, 50 mg/kg) exhibits significant antitumor activities in mice HT29 xenograft tumors[1].
MLN0905 (p.o.; 0-14.5 mg/kg; daily, QD×3/week) has marked antitumor effects in kinds of lymphoma xenograft model[1][2].
| Catalog Number | I000899 |
| CAS Number | 1228960-69-7 |
| Synonyms | 2-[[5-[3-(dimethylamino)propyl]-2-methylpyridin-3-yl]amino]-9-(trifluoromethyl)-5,7-dihydropyrimido[5,4-d][1]benzazepine-6-thione |
| Molecular Formula | C24H25F3N6S |
| Purity | ≥95% |
| InChI | InChI=1S/C24H25F3N6S/c1-14-19(9-15(12-28-14)5-4-8-33(2)3)31-23-29-13-16-10-21(34)30-20-11-17(24(25,26)27)6-7-18(20)22(16)32-23/h6-7,9,11-13H,4-5,8,10H2,1-3H3,(H,30,34)(H,29,31,32) |
| InChIKey | CODBZFJPKJDNDT-UHFFFAOYSA-N |
| SMILES | CC1=C(C=C(C=N1)CCCN(C)C)NC2=NC=C3CC(=S)NC4=C(C3=N2)C=CC(=C4)C(F)(F)F |
| Reference | [1]. Duffey MO, et al. Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905). J Med Chem. 2012 Jan 12;55(1):197-208. [2]. Shi JQ, et al. MLN0905, a small-molecule plk1 inhibitor, induces antitumor responses in human models of diffuse large B-cell lymphoma. Mol Cancer Ther. 2012 Sep;11(9):2045-53. |
