| 生物活性 | BS-194 is an orally active, selective and potentCDKinhibitor. BS-194 inhibitsCDK2,CDK1,CDK5,CDK7,CDK9(IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibitscancercells proliferation. BS-194 can be used in the research of cancers like breastcancer, coloncancer[1]. |
| IC50& Target[1] | CDK2 3 nM (IC50) | CDK1 30 nM (IC50) | CDK5 30 nM (IC50) | CDK7 250 nM (IC50) | CDK9 90 nM (IC50) |
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体外研究
(In Vitro) | BS-194 (compound 4k, 72 h) inhibits various cancer cells (MCF-7, MDA-MB-231, MCF-10A, CPLO-205, HCT-116, A549, SaOS2, PC3 ,HepG2, SK-Ov-3) growth, with IC50values ranging from 100 nM to 1 μM[1].
BS-194 (10 μM, 24 h) promotes cell cycle arrest in in S and G2/M phases in HCT116 cells[1].
BS-194 (10 μM, 24 h) inhibits phosphorylation of CDK substrates, and promotes cyclin loss in HCT116 cells[1].
Cell Cycle Analysis[1] | Cell Line: | HCT116 | | Concentration: | 0, 0.01, 0.1, 1, 10 μM | | Incubation Time: | 24 h | | Result: | Showed a significant reduction in G1, and increased in S and G2/M phases. |
Western Blot Analysis[1] | Cell Line: | HCT116 | | Concentration: | 0, 0.1, 10, 20 μM | | Incubation Time: | 0, 0.1, 10, 20 μM | | Result: | Inhibited the phosphorylation of the CDK2 substrate RB (retinoblastoma) at Ser-780, Ser-795, Ser-801, Ser-807/Ser-811, and Thr-821.
Inhibited levels of cyclin A, cyclin B, and cyclin D1.
Inhibited phosphorylation of Thr-170 of CDK2. |
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体内研究
(In Vivo) | 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). |
| 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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