您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > PI3kδinhibitor 1
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PI3kδinhibitor 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PI3kδinhibitor 1图片
CAS NO:1332075-63-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
PI3kδ inhibitor 1 是一种有效的选择性PI3Kδ抑制剂,IC50为 3.8 nM。
生物活性

PI3kδ inhibitor1 is a potent and selectivePI3Kδinhibitor with anIC50of 3.8 nM.

IC50& Target[3]

PI3Kδ

3.8 nM (IC50)

体外研究
(In Vitro)

PI3kδ inhibitor 1 (Compound 3) is a potent inhibitor of PI3Kδ that is 200-400 fold selective for all three remaining Class I PI3K isoforms and extremely selective relative to 239 kinases tested in SelectScreen service (0/239 kinases showing >50% inhibition when tested at 1 μM; mTOR, DNA-PK, VPS34, PI4Kα and PI4Kβ are inhibited at 10% or less when tested at 1 μM; PIKC2A and PIKC2B are inhibited at 11% and 42%, respectively, at this same concentration and show less than 10% inhibition when tested at 0.1 μM; the PIKK family kinases ATM and ATR are not assessed)[1].

体内研究
(In Vivo)

The pharmacokinetic properties of PI3kδ inhibitor 1 (Compound 3) are evaluated in mice and rats when dosed IV and orally. Good plasma exposures and reasonable half-lives are observed upon oral dosing, a reflection of high oral bioavailability (80% and 90% at a low dose for mouse and rat, respectively), moderate volume of distribution, and moderate clearance. PI3kδ inhibitor 1 has moderate terminal elimination half-life (t1/2=2.6 h, 2.9 h, 5 h, 2.6, 3.8 and 4.8 h for mouse (5 mg/kg, po), mouse (20 mg/kg, po), mouse (40 mg/kg, po), rat (5 mg/kg, po), rat (10 mg/kg, po), rat (30 mg/kg, po)). Plasma exposures and Cmax levels increase with dose in both mice and rats, important in that inflammatory disease models utilize these two species. Plasma protein binding for PI3kδ inhibitor 1 ranges from 80-88% in rodents and is consistent with values obtained in human plasma (86%)[1].

分子量

504.60

Formula

C28H33FN6O2

CAS 号

1332075-63-4

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.