P62-RNF168 agonist-1 (12.5-100 mg/kg, i.p., single dose) has an MTD of 50 mg/kg in BALB/c mice, while in female nude mice, the MTD is 12.5 mg/kg[1].
P62-RNF168 agonist-1 (5-10 mg/kg, i.p., single every 3 days for 22 days) promotes tumor apoptosis and inhibits tumor growth in mice[1].
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Pharmacokinetic Parameters of Antitumor agent-81 in Female BALB/c nude mice[1].
| Dose | T1/2 (h) | Cmax (ng/mL) | AUC0-t (h?ng/mL) | CL ((mL/h)/kg) |
| IP (5 mg/kg) | 16.17 | 26.10 | 215.69 | 19647.83 |
| IP (10 mg/kg) | 31.00 | 39.87 | 408.18 | 16554.30 |
| IP (20 mg/kg) | 22.10 | 52.23 | 1003.58 | 14669.81 |
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| Animal Model: | Female BALB/c nude mice (xenograft tumor model)[1]. |
| Dosage: | 5, 10 mg/kg |
| Administration: | Intraperitoneal injection; single every 3 days for 22 days |
| Result: | Suppressed tumor growth by promoting apoptosis in xenografted tumorigenesis. |
| Animal Model: | Female BALB/c nude mice[1]. |
| Dosage: | 5, 10, 20 mg/kg |
| Administration: | Intraperitoneal injection; single |
| Result: | Exhibited plasma concentration peaked 1 h after administration.
Showed a relatively high maximum concentration (Cmax= 52.23 ng/mL) and exposure (AUC0-t= 1003.58 h?ng/mL) at a dose of 20 mg/kg.
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| Animal Model: | BALB/c mice, Female nude mice[1] |
| Dosage: | 25, 50, 75, 100 mg/kg, single dose; 12.5, 25, 50 mg/kg, single dose |
| Administration: | Intraperitoneal injection |
| Result: | Showed in the 100 mg/kg dosage group of BALB/c mice, out of 8 animals, 3 males and 3 females died on the 7th day, and the remaining animals experienced diarrhea. In the 75 mg/kg dosage group, 1 out of 8 animals (1 male) had diarrhea on the 7th day. There were no deaths or diarrhea observed in the ≤50 mg/kg dosage group.
Showed in the female nude mice, both the 25 and 50 mg/kg dosage groups experienced deaths or diarrhea, while the 12.5 mg/kg dosage group had no deaths or diarrhea. |
