PI3K/mTOR Inhibitor-4

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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。

CAS NO:

2361215-32-7

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
25mg	询价
50mg	询价
100mg	询价

PI3K/mTOR Inhibitor-4 是一种泛 I 类 PI3K/mTOR 抑制剂，具有口服活性。PI3K/mTOR Inhibitor-4 对 PI3Kα、PI3Kγ、PI3Kδ 和 mTOR 具有酶抑制活性，IC50 值分别为 0.63 nM、22 nM、9.2 nM 和 13.85 nM。PI3K/mTOR Inhibitor-4 可用于癌症的研究。

Cas No.

2361215-32-7

分子式

C₂₇H₂₂FN₃O₆S

分子量

535.54

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

PI3K/mTOR Inhibitor-4 is an orally active pan-class IPI3K/mTORinhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR withIC₅₀values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer^[1].

PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC₅₀values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively^[1].
PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC₅₀values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively^[1].
PI3K/mTOR Inhibitor-4 (2.5-10 µM; 24 h) inhibits the PI3K/AKT/mTOR pathway^[1].

Cell Viability Assay^[1]

Cell Line:	PC12 and LO2 cells
Concentration:	0.625-20 µM
Incubation Time:	72 h
Result:	Showed low toxicity in concentrations from 0.625 µM to 20 µM.

Western Blot Analysis^[1]

Cell Line:	Hela cells
Concentration:	2.5, 5 and 10 µM
Incubation Time:	24 h
Result:	Dose-dependently decreased the level of phosphorylation of AKT and its downstream target S6 in Hela cell line.

PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague-Dawley rats^[1].
PI3K/mTOR Inhibitor-4 (oral; 10-50 mg/kg) shows significant efficiency in Hela/A549 tumor xenograft models without causing significant weight loss and toxicity^[1].

Animal Model:

SD rats (male; 200-220 g)^[1]

Dosage:

1, 10 mg/kg

Administration:

Intravenous, oral

Result:

IV (1 mg/kg)	PO (10 mg/kg)
CL (ml/min/kg)	Vss (ml/kg)	T_max(h)	C_max(ng/ml)	AUCinf (ng*h/ml)	t_1/2(h)	F(%)
8.6	1199.81	2.67	886.67	4753.35	1.78	24.1

Animal Model:	BALB/c nude mice (female; 6-7 weeks; 18-22 g)^[1]
Dosage:	10, 20, 40, 50 mg/kg/d (Hela model) and 20, 40 mg/kg/d (A549 model)
Administration:	Oral
Result:	Inhibited the growth of xenograft tumors in a dose-dependent manner.