CAS:957054-30-7GDC-0941

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Synonyms: RG 7321;Pictilisib

GDC-0941 is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β(11-fold) and p110γ(25-fold).

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18817579266

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18817579266

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实验数据

技术信息

CAS号

957054-30-7

储存条件

分子式

C23H27N7O3S2

运输

蓝冰

分子量

513.64

别名

RG 7321;Pictilisib

溶解度

DMSO	80.0 mg/mL (155.8 mM)
Water	insoluble

动物实验配方

2% DMSO+30% PEG 300+5% Tween 80+water

5 mg/mL

生物活性

靶点 p110β

IC50:33nM p110γ

IC50:75nM PI3Kα

IC50:3nM PI3Kδ

IC50:3nM
描述Phosphatidylinositol-3-kinases (PI3Ks) are lipid kinases that catalyze the phosphorylation of the 3-hydroxyl position of phosphatidylinositides and participate in several cellular process. Up to now, there are eight PI3 kinases have been identified, which are divided into classes IA, 1B, II, and III based on the sequence homology and substrate preference. GDC-0941 is a potent, selective and orally bioavailable inhibitor of class I PI3Ks (p110α IC50=3nM, p110δ IC50=3nM, p110β IC50=33nM, p110γ IC50=75nM, measured by scintillation proximity assay), with less potency to mTOR (IC50=0.58μM, measured by HTRF assay)^[1]. GDC-0941 is a derivative of PI-103, a dual PI3K/mTOR inhibitor, and has good pharmacokinetic properties. Its oral bioavailability is up to 78% in subcutaneous U-87 MG xenograft mice and shows sustained and remarkable inhibition of Akt phosphorylation and tumor growth, up to 98%^[2]. GDC-0941 barely penetrated through the intact BBB^[3].
作用机制GDC-0941 is a potent, ATP competitive inhibitor of p110α with Ki value of 10.2±4.4 nM.^[1]
动物研究
剂量
Mice: min = 75 mg/kg^[4], max = 150 mg/kg^[5] Nude Mice: min = 25 mg/kg bid, max = 50 mg/kg bid^[6]

给药途径
p.o

动物研究
剂量	Mice: min = 75 mg/kg^[4], max = 150 mg/kg^[5] Nude Mice: min = 25 mg/kg bid, max = 50 mg/kg bid^[6]
给药途径	p.o