产品
编 号：F756341
分子式：C26H38N6O3
分子量：482.62
分子式：C26H38N6O3
分子量：482.62
产品类型
规格
价格
是否有货
结构图
CAS No: 2848632-52-8
产品详情
生物活性：
Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model.
体内研究：
Antitumor agent-101 (Compound 27) (2 mg/kg，腹腔注射，每周五天) 通过抑制 G9a/GLP 的甲基转移酶活性来抑制 PANC-1 异种移植肿瘤的生长。Antitumor agent-101 (2 mg/kg，腹腔注射) 显示 Cmax 为 316 ng/mL，平均停留时间 (MRT) 为 0.61 小时。Animal Model:PANC-1 xenograft tumor models in male Balb/c nu/nu mice
Dosage:2 mg/kg
Administration:Intraperitoneal injection (i.p.), 5 days a week (5 days on and 2 days off).
Result:Exhibited potent antitumor activity with a tumor growth inhibition (TGI) rate of 52.2% with no obvious toxicity. Showed lower levels of H3K9me2 than the vehicle group.
Animal Model:Male ICR Mice (Pharmacokinetic assay)
Dosage:2 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result: Pharmacokinetic parameters for antitumor agent-101 (Compound 27) in rats RouteDose (mg/kg)Cmax (ng/mL)AUC0-t (h?ng/mL) AUC0-? (h?ng/mL)MRT (h)
i.p.23162082140.61
体外研究：
Antitumor agent-101 (Compound 27) ( 0-5 μM；48 小时) 抑制 PANC-1 和 MDA-MB-231 细胞的增殖和克隆形成。Antitumor agent-101 ( 0-10 μM；0-96 小时) 以浓度和时间依赖性方式有效降低 PANC-1 和 MDA-MB-231 细胞中的 H3K9me2 水平。
Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model.
体内研究：
Antitumor agent-101 (Compound 27) (2 mg/kg，腹腔注射，每周五天) 通过抑制 G9a/GLP 的甲基转移酶活性来抑制 PANC-1 异种移植肿瘤的生长。Antitumor agent-101 (2 mg/kg，腹腔注射) 显示 Cmax 为 316 ng/mL，平均停留时间 (MRT) 为 0.61 小时。Animal Model:PANC-1 xenograft tumor models in male Balb/c nu/nu mice
Dosage:2 mg/kg
Administration:Intraperitoneal injection (i.p.), 5 days a week (5 days on and 2 days off).
Result:Exhibited potent antitumor activity with a tumor growth inhibition (TGI) rate of 52.2% with no obvious toxicity. Showed lower levels of H3K9me2 than the vehicle group.
Animal Model:Male ICR Mice (Pharmacokinetic assay)
Dosage:2 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result: Pharmacokinetic parameters for antitumor agent-101 (Compound 27) in rats RouteDose (mg/kg)Cmax (ng/mL)AUC0-t (h?ng/mL) AUC0-? (h?ng/mL)MRT (h)
i.p.23162082140.61
体外研究：
Antitumor agent-101 (Compound 27) ( 0-5 μM；48 小时) 抑制 PANC-1 和 MDA-MB-231 细胞的增殖和克隆形成。Antitumor agent-101 ( 0-10 μM；0-96 小时) 以浓度和时间依赖性方式有效降低 PANC-1 和 MDA-MB-231 细胞中的 H3K9me2 水平。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备