产品名称

Duvelisib (IPI-145, INK1197)

一般描述

Duvelisib is a novel and selective PI3K δ/γ inhibitor.

别 称

8-chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]isoquinolin-1-one

纯 度

≥98.0%(HPLC)

CAS NO.

1201438-56-3

分子式

C²²H¹⁷ClN⁶O

分子量

416.869

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Duvelisib is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. Upon administration, duvelisib prevents the activation of the PI3K delta/gamma-mediated signaling pathways which may lead to a reduction in cellular proliferation in PI3K delta/gamma-expressing tumor cells. Unlike other isoforms of PI3K, the delta and gamma isoforms are overexpressed primarily in hematologic malignancies and inflammatory and autoimmune diseases. By selectively targeting these PI3K isoforms, PI3K signaling in normal, non-neoplastic cells is minimally or not affected which would result in a more favorable side effect profile.

Duvelisib is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov