| Bioactivity | Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC50 of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity[1]. |
| Target | IC50: 21.9 nM in MNNG/HOS cells |
| Invitro | Antitumor agent-51 (compound R-8i) (0-20 μM; 72 hours) selectively inhibits MNNG/HOS OS cells proliferation with IC50=21.9 nM, and has much less inhibitory activity on two normal BMSC and GES1 cells (IC50>10 μM)[1].Antitumor agent-51 (5 nM; 24 hours) induces a cell cycle arrest in MNNG/HOS cells with a 23% increase in G0/G1 phase, but no apparent cell apoptosis[1].Antitumor agent-51 (5 and 20 nM; 24 hours) significantly suppresses the migration of MNNG/HOS cells[1]. Cell Proliferation Assay Cell Line: |
| In Vivo | Antitumor agent-51 (12.5 or 62.5 mg/kg; i.p. or i.v., single) exhibits good intraperitoneal plasma exposures (AUC0-∞>6900 h ng/mL) and an acceptable bioavailability (52.1%) for the i.p. administration in male ICR mice[1].Antitumor agent-51 (62.5 mg/kg; i.p., twice per day for 18 days) significantly suppresses MNNG/HOS tumor growth with tumor growth inhibition (TGI) of 52.9% and does not induce an obvious toxicity in nude mice[1].Pharmacokinetic Parameters of Antitumor agent-51 in male ICR mice[1]. |
| Name | Antitumor agent-51 |
| Formula | C23H25N5O2S |
| Molar Mass | 435.54 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Deng Y, et al. Novel 2-phenyl-3-(Pyridin-2-yl) thiazolidin-4-one derivatives as potent inhibitors for proliferation of osteosarcoma cells in vitro and in vivo. Eur J Med Chem. 2022;228:114010. |