Avagacestat (BMS-708163)
中文名称：塞来西布
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
客户使用Selleck的Avagacestat (BMS-708163)发表文献22篇
客户使用该产品的4个实验数据
产品质控
Avagacestat (BMS-708163)相关产品
| 相关靶点 | gamma-secretase | 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 |
Secretase抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 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 | 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。 | ||||
|---|---|---|---|---|---|
| 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 |
|
| 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 |
|---|---|---|---|---|---|
| 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 |
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) | |||
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体外溶解度 |
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 |
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体内溶解度 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
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）
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）
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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