产品
编 号：F755756
分子式：C19H19N7O3
分子量：393.4
分子式：C19H19N7O3
分子量：393.4
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: 2765180-17-2
产品详情
生物活性：
Antitumor agent-81 (compound 5a) is a low cytotoxic P62-RNF168 agonist that promotes the interaction of P62 with RNF168. Antitumor agent-81 induces a decrease in RNF168-mediated H2A ubiquitination and impairs homologous recombination-mediated DNA repair. Antitumor agent-81 also inhibits mice xenograft tumor growth in a dose-dependent manner.
体内研究：
Antitumor agent-81 (5, 10 mg/kg; i.p.; single every 3 days for 22 days) suppresses tumor volumes in a dose-dependent manner in mice.1.19Pharmacokinetic Parameters of Antitumor agent-81 in Female BALB/c nude mice.DoseT1/2 (h)Cmax (ng/mL)AUC0-t (h?ng/mL)CL ((mL/h)/kg)
IP (5 mg/kg)16.1726.10215.6919647.83IP (10 mg/kg)31.0039.87408.1816554.30IP (20 mg/kg)22.1052.231003.5814669.81Animal Model:Female BALB/c nude mice (xenograft tumor model).
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.
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.
体外研究：
Antitumor agent-81 (0-20 μM; 72 h) exhibits antiproliferative activity in cells of the most common cancer types.Antitumor agent-81 (1, 2, 5 μM; 24 h) compromises HR (homologous recombination)-mediated DSB repair in HCT-116 cells.Antitumor agent-81 tethers the interaction between P62 and RNF168 in HCT-116 cells.Antitumor agent-81 inhibits the catalytic activity of RNF168 and RNF168 E3 ligase activity in HCT-116 cells.
Antitumor agent-81 (compound 5a) is a low cytotoxic P62-RNF168 agonist that promotes the interaction of P62 with RNF168. Antitumor agent-81 induces a decrease in RNF168-mediated H2A ubiquitination and impairs homologous recombination-mediated DNA repair. Antitumor agent-81 also inhibits mice xenograft tumor growth in a dose-dependent manner.
体内研究：
Antitumor agent-81 (5, 10 mg/kg; i.p.; single every 3 days for 22 days) suppresses tumor volumes in a dose-dependent manner in mice.1.19Pharmacokinetic Parameters of Antitumor agent-81 in Female BALB/c nude mice.DoseT1/2 (h)Cmax (ng/mL)AUC0-t (h?ng/mL)CL ((mL/h)/kg)
IP (5 mg/kg)16.1726.10215.6919647.83IP (10 mg/kg)31.0039.87408.1816554.30IP (20 mg/kg)22.1052.231003.5814669.81Animal Model:Female BALB/c nude mice (xenograft tumor model).
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.
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.
体外研究：
Antitumor agent-81 (0-20 μM; 72 h) exhibits antiproliferative activity in cells of the most common cancer types.Antitumor agent-81 (1, 2, 5 μM; 24 h) compromises HR (homologous recombination)-mediated DSB repair in HCT-116 cells.Antitumor agent-81 tethers the interaction between P62 and RNF168 in HCT-116 cells.Antitumor agent-81 inhibits the catalytic activity of RNF168 and RNF168 E3 ligase activity in HCT-116 cells.
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