aladdin 阿拉丁 P408161 PFI-1 (PF-6405761) 1403764-72-6 10mM in DMSO

中文名：PFI-1 (PF-6405761)

英文名：PFI-1 (PF-6405761)

英文别名：Benzenesulfonamide, 2-methoxy-N-(1,2,3,4-tetrahydro-3-methyl-2-oxo-6-quinazolinyl)-

纯度：10mM in DMSO

货号：P408161

包装：1ml

Cas号：1403764-72-6

存储温度：-80℃储存

产品介绍：

Information

PFI-1 (PF-6405761) PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.
In vitro

PFI-1 binds to with cyclic AMP response binding protein with K_D of 49 μM. PFI-1 has an EC50 of 1.89 μM for the inhibition of IL6 production from human blood mononuclear cells stimulated by LPS. PFI-1 induces dose-dependent reduction of cell viability in T4302 CD133+ cells. PFI-1 inhibits the proliferating of three NET cell lines (Bon-1 derived from a pancreatic NET, and H727 and H720 derived from lung NETs).

In vivo

PFI-1 administrated (1 mg/kg i.v.) in the rat results in the volume of distribution of 1 L/kg, the plasma clearance of 18/mL·min^–1·kg^–1 and half-life of 1 hour. PFI-1 oral dosed (2 mg/kg) in the rat results in the oral bioavailability as low as 32%. PFI-1 administrated (2 mg/kg s.c.) in the mouse results in a C_max of 58 ng/mL with a T_max of 1 h and a half-life of approximately 2 hours.
Cell Data

cell lines：

Concentrations：1 mM

Incubation Time：5 days

Powder Purity:≥96%

查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/P408161.html