产品
编 号：F032996
分子式：C20H27N5O3
分子量：385.46
分子式：C20H27N5O3
分子量：385.46
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1092443-55-4
产品详情
生物活性：
BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer.
体内研究：
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.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.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.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.Animal Model:Nude mice bearing MCF-7 cell
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
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)
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 30147
p.o. 10 88 15178
administration routedose (mg/kg)T1/2 (min) Cl (mL/min/kg) Vz
i.v. 10 210 5 1391
体外研究：
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 IC50 values ranging from 100 nM to 1 μM.BS-194 (10 μM, 24 h) promotes cell cycle arrest in in S and G2/M phases in HCT116 cells.BS-194 (10 μM, 24 h) inhibits phosphorylation of CDK substrates, and promotes cyclin loss in HCT116 cells.
BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer.
体内研究：
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.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.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.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.Animal Model:Nude mice bearing MCF-7 cell
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
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)
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 30147
p.o. 10 88 15178
administration routedose (mg/kg)T1/2 (min) Cl (mL/min/kg) Vz
i.v. 10 210 5 1391
体外研究：
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 IC50 values ranging from 100 nM to 1 μM.BS-194 (10 μM, 24 h) promotes cell cycle arrest in in S and G2/M phases in HCT116 cells.BS-194 (10 μM, 24 h) inhibits phosphorylation of CDK substrates, and promotes cyclin loss in HCT116 cells.
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