BS-194 (compound 4K, intraperitoneal injection, 5 or 10 mg/kg, twice daily for 14 days) inhibits tumor growth with no apparent toxicity in MCF-7 tumor xenografts[1].
BS-194 (i.p., i.v., p.o., 10 mg/kg) is orally bioavailable, with elimination half-lives of 147 min (i.p.), 210 min (i.v.), and 178 min (p.o.) respectively[1].
BS-194 (oral gavage, 25 mg/mL) reduces rapid RB and PolII (RNA polymerase II) phosphorylation, but recovery within 24 h in nu/nu-BALB/c athymic nude mice[1].
BS-194 (oral gavage, 25 mg/kg, daily for 14 days) inhibits tumor growth in HCT116 tumor xenografts, with no significant loss in animal weights[1].
| Animal Model: | Nude mice bearing MCF-7 cell[1] |
| Dosage: | 5 or 10 mg/kg, twice daily for 14 days. |
| Administration: | Intraperitoneal injection |
| Result: | Inhibited tumor growth in a dose-dependent manner (30% and 40% reduction at 5 and 10 mg/kg dose, respectively). |
| Animal Model: | HCT116 tumor xenografts[1] |
| Dosage: | 25 mg/kg, daily for 14 days. |
| Administration: | Oral gavage |
| Result: | Inhibited tumor growth by 50% reduction at 25 mg/kg.
Decreased levels of Rb phosphorylation at Ser807/811 and Thr821 (in resected tumors).
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| Animal Model: | Mice (pharmacokinetic assay)[1] |
| Dosage: | 10 mg/kg |
| Administration: | Intraperitoneal injection, intravenous injection, oral administration |
| Result: | Pharmacokinetic profile of BS-194 (compound 4k).
| administration route | dose (mg/kg) | bioavail-ability (%) | Cmax (min) | T1/2 (min) | | i.p. | 10 | 73 | 30 | 147 | | p.o. | 10 | 88 | 15 | 178 | | administration route | dose (mg/kg) | T1/2 (min) | Cl (mL/min/kg) | Vz | | i.v. | 10 | 210 | 5 | 1391 |
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