Avagacestat (BMS-708163)

中文名称：塞来西布

目录号：S1262 Purity: 99.63%

Avagacestat (BMS-708163)是口服生物有效的，选择性的γ-分泌酶抑制剂，作用于Aβ40和Aβ42时，IC50分别为0.3 nM和0.27 nM，比作用于Notch选择性高193倍。Phase 2。

Avagacestat (BMS-708163) Chemical Structure

CAS: 1146699-66-2

规格	价格	库存
5mg	1403.72	现货
10mg	2620.13	现货
50mg	7967.17	现货
200mg	15700	现货
1g	39900	现货
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产品质控

批次：纯度： 99.63%

99.63

Avagacestat (BMS-708163)相关产品

相关靶点	gamma-secretase	点击展开
相关产品	DAPT RO4929097 DBZ (Dibenzazepine) LY411575 MK-0752 Semagacestat (LY450139) Nirogacestat (PF-03084014) MDL-28170 L-685,458	点击展开
相关化合物库	FDA药物库天然产物库已知活性药物库-I 蛋白酶抑制剂库泛素化化合物库	点击展开

细胞实验数据示例

细胞系	实验类型	孵育时间	活性描述	文献信息
human IMR32 cell	Function assay	2 h	Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA, IC50=0.13 nM	23312944
human IMR32 cell	Function assay	2 h	Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA, IC50=1.5 nM	23312944
human H4 cells	Function assay		Inhibition of gamma secretase-mediated amyloid beta42 production in human H4 cells expressing human APP swedish mutant, IC50=0.225 μM	22420884
HEK293 cells	Function assay		Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis, IC50=1.2 nM	23312944
CHO cells	Function assay		Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA, ED50=1.2 nM	23713656
human 786-0 cell	Growth inhibition assay		Inhibition of human 786-0 cell growth in a cell viability assay, IC50=0.32173 μM	SANGER
human NCI-H810 cell	Growth inhibition assay		Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=0.42598 μM	SANGER
human IGR-1 cell	Growth inhibition assay		Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=1.04778 μM	SANGER
human SK-MEL-3 cell	Growth inhibition assay		Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=1.49922 μM	SANGER
human HT-1080 cell	Growth inhibition assay		Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=2.48764 μM	SANGER
human NCI-H23 cell	Growth inhibition assay		Inhibition of human NCI-H23 cell growth in a cell viability assay, IC50=3.9322 μM	SANGER
human Calu-6 cell	Growth inhibition assay		Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=4.96014 μM	SANGER
human CAPAN-1 cell	Growth inhibition assay		Inhibition of human CAPAN-1 cell growth in a cell viability assay, IC50=5.17886 μM	SANGER
human COLO-668 cell	Growth inhibition assay		Inhibition of human COLO-668 cell growth in a cell viability assay, IC50=5.40221 μM	SANGER
human TE-6 cell	Growth inhibition assay		Inhibition of human TE-6 cell growth in a cell viability assay, IC50=6.19082 μM	SANGER
human LCLC-97TM1 cell	Growth inhibition assay		Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=10.0886 μM	SANGER
human CAS-1 cell	Growth inhibition assay		Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=13.671 μM	SANGER
human RPMI-2650 cell	Growth inhibition assay		Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50=13.8124 μM	SANGER
human MDA-MB-157 cell	Growth inhibition assay		Inhibition of human MDA-MB-157 cell growth in a cell viability assay, IC50=14.2431 μM	SANGER
human KINGS-1 cell	Growth inhibition assay		Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50=14.3762 μM	SANGER
human BB49-HNC cell	Growth inhibition assay		Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=14.4138 μM	SANGER
human SK-UT-1 cell	Growth inhibition assay		Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=14.6882 μM	SANGER
human EW-11 cell	Growth inhibition assay		Inhibition of human EW-11 cell growth in a cell viability assay, IC50=14.8832 μM	SANGER
human D-502MG cell	Growth inhibition assay		Inhibition of human D-502MG cell growth in a cell viability assay, IC50=14.9034 μM	SANGER
human MMAC-SF cell	Growth inhibition assay		Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50=15.0833 μM	SANGER
human NCI-H1648 cell	Growth inhibition assay		Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=15.778 μM	SANGER
human NCI-H292 cell	Growth inhibition assay		Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50=15.8806 μM	SANGER
human NMC-G1 cell	Growth inhibition assay		Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=16.6293 μM	SANGER
human SAS cell	Growth inhibition assay		Inhibition of human SAS cell growth in a cell viability assay, IC50=17.7812 μM	SANGER
human HCT-116 cell	Growth inhibition assay		Inhibition of human HCT-116 cell growth in a cell viability assay, IC50=18.7965 μM	SANGER
human SBC-5 cell	Growth inhibition assay		Inhibition of human SBC-5 cell growth in a cell viability assay, IC50=19.03 μM	SANGER
点击查看更多细胞系数据

生物活性

产品描述

特性

BMS-708163作用于Notch过程似乎比semagacestat (LY450139)效果要好，且所需量要少

靶点

Aβ42 ^[1] (in H4-8Sw cells)	Aβ40 ^[1] (in H4-8Sw cells)
0.27 nM	0.3 nM

体外研究(In Vitro)
体外研究活性	BMS-708163 抑制Notch 过程时显示出低选择性。 ^[1]

体内研究(In Vivo)
体内研究活性	鼠和犬口服处理BMS-708163 明显且长期降低脑，血浆，脑脊液中的Aβ40 水平。BMS-708163作用于犬时，没有剂量限制影响(用3 mg/kg BMS-708163处理6个月内的犬)。^[1]
动物实验	Animal Models	雌性Harlan Sprague Dawley鼠或 ATM-405-142K9，7到10月大的 naïve II级犬。
	Dosages	10 mg/kg (鼠) 或2.5 mg/kg (犬)
	Administration	每天口服饲喂

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT01002079	Completed	Alzheimer Disease	Bristol-Myers Squibb\|PRA Health Sciences	August 2010	Phase 1
NCT01057030	Completed	Alzheimer Disease	Bristol-Myers Squibb	March 2010	Phase 1
NCT01042314	Completed	Alzheimer Disease	Bristol-Myers Squibb	January 2010	Phase 1
NCT01039194	Completed	Alzheimer Disease	Bristol-Myers Squibb	January 2010	Phase 1
NCT00979316	Completed	Alzheimer Disease	Bristol-Myers Squibb	September 2009	Phase 1
NCT00890890	Terminated	Alzheimer''s Disease	Bristol-Myers Squibb	May 2009	Phase 2

参考文献
[1] Gillman KW, et al. Med Chem Lett, 2010, 1 (3), 120–124.

参考文献

[1] Gillman KW, et al. Med Chem Lett, 2010, 1 (3), 120–124.

化学信息&溶解度

分子量	520.88	分子式	C₂₀H₁₇ClF₄N₄O₄S
CAS号	1146699-66-2	SDF	Download Avagacestat (BMS-708163) SDF
Smiles	C1=CC(=CC=C1S(=O)(=O)N(CC2=C(C=C(C=C2)C3=NOC=N3)F)C(CCC(F)(F)F)C(=O)N)Cl
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 104 mg/mL ( (199.66 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (191.98 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 104 mg/mL ( (199.66 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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* 必填项

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