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Avagacestat
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。
Avagacestat图片
CAS NO:1146699-66-2
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
BMS-708163
产品介绍
AvagaceSTAT 是一种有效的γ-secretase抑制剂,抑制 Aβ42 (IC50:0.27 nM) 和 Aβ40 (IC50:0.30 nM) 的产生。它同时抑制 Notch 胞内结构域 (NICD) (IC50:0.84 nM) 和 CYP2C19 (IC50:20 nM) 。它可用于阿尔兹海默症的研究。

产品描述

Avagacestat (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.

体外活性

BMS-708163 exhibits weaker selectivity for inhibition of Notch processing with 193-fold IC50 value. [1]

体内活性

Oral administration of BMS-708163 significantly reduces Aβ40 levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs. BMS-708163 has no dose-limiting effects in dogs (3 mg/kg during 6 months), with a high brain to plasma ratio (2.4). [1]

细胞实验

BMS-708163 is dissolved in DMSO. The cell viability is assessed using a tetrazolium salt (WST-8)-based colorimetric assay from the Cell Counting Kit 8 (CCK-8). The cells are seeded into 96-well plates at an initial density of 5×103 cells/well and cultured for 24?h, after which the cells are cultured with DMSO, increased concentrations of gefitinib or BMS708163, BIBW2992, or the combination of BMS708163 and BIBW2992 for an additional 48?h. The A450 is measured in a microplate reader after 10?μL of CCK-8 solution is added and incubated for 1?h. The percentage of growth is shown relative to untreated controls.

Cas No.

1146699-66-2

分子式

C20H17ClF4N4O4S

分子量

520.88

别名

BMS-708163

储存和溶解度

H2O:<1 mgml
Ethanol:<1 mgml
DMSO:96 mg/mL (184.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years