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- 2025年12月05日
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3035774-65-0
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Antitumor agent-51
MCE 国际站：Antitumor agent-51
产品活性：Antitumor agent-51 对骨肉瘤细胞的生长和迁移具有有效的选择性抑制作用，对 MNNG/HOS 细胞的 IC50 为 21.9 nM。Antitumor agent-51 具有低毒性和相当大的生物利用度。
研究领域：Others
作用靶点：Others
In Vitro: 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).
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.
Antitumor agent-51 (5 and 20 nM; 24 hours) significantly suppresses the migration of MNNG/HOS cells.
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.
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.
Pharmacokinetic Parameters of Antitumor agent-51 in male ICR mice.
| IV (12.5 mg/kg) | IP (62.5 mg/kg) | |
| T1/2 (h) | 0.061 | 0.641 |
| AUC0-inf (h·ng/mL) | 3230 | 8406 |
| Cmax (ng/mL) | 20511 | |
| CL (mL/min/kg) | 66.9 | |
| F (%) | 52.1 |
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