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抑制剂 > p13k/Akt/mTOR 信号传导 > PF-05212384 (PKI-587)
产品名称:
PF-05212384 (PKI-587)
型号:
CS-01Y70710
生产地址
进口、国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

25mg

CAS

1197160-78-3

别名

 

化学名

1-[4-[4-(dimethylamino)piperidine-1-carbonyl]phenyl]-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea

分子式

C32H41N9O4

分子量

615.73

溶解度

15.4mg/mL in DMSO with gentle warming

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

PF-05212384 is an inhibitor of PI3K/mTOR with IC50 values of 0.4nM, 6nM, 8nM, 6nM and 1.4nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively [1].

PF-05212384 is a pan-PI3K/mTORinhibitor and shows to be highly selective for PI3K and mTOR. Besides the wt P13K, PF-05212384 can also inhibit mutant P13K with IC50 values of 0.6nM for both H1047R and E545K mutants. In cellular assay, PF-05212384 potently inhibits tumor growth in MDA-361 and PC3-MM2 cell lines with IC50 values of 4nM and 13.1nM, respectively. Meanwhile, PF-05212384 suppresses the phosphorylation of PI3K/mTOR signaling pathway proteins in cells. It inhibits the phosphorylation of Akt as well as the Akt effector proteins including GSK3 kinase, ENOS and PRAS 40. Moreover, PF-05212384 has potent anti-tumor activity in a variety of xenograft models including H1975, BT474, HCT116, H1975 and U87MG [1, 2]

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:PF-05212384 (PKI-587) 

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