Avagacestat (BMS-708163)

For research use only. Not for use in humans.

目录号:S1262 中文名称:塞来西布

Avagacestat (BMS-708163) Chemical Structure

CAS No. 1146699-66-2

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Aβ40Aβ42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。

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客户使用Selleck生产的Avagacestat (BMS-708163)发表文献20篇:

产品安全说明书

Gamma-secretase抑制剂选择性比较

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Aβ40Aβ42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
γ secretase(Aβ42) [1]
(in H4-8Sw cells)
γ secretase(Aβ40) [1]
(in H4-8Sw cells)
0.27 nM 0.3 nM
体外研究

BMS-708163 抑制Notch 过程时显示出低选择性。 [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human IMR32 cell MoPPSpVv[3Srb36gZZN{[Xl? NEfIVYczKGh? M3Pyc2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIHj1cYFvKEmPUkOyJINmdGxibXXtZpJidmVidYPpcochSVCSIHHzJJN2[nO2cnH0[UBi\nSncjCyJIhzeyCkeTDFUGlUSSxiSVO1NF0xNjF|IH7N M1TQfFI{OzF{OUS0
human H4 cells MkPnSpVv[3Srb36gZZN{[Xl? M{HPe2lvcGmkaYTpc44hd2ZiZ3HtcYEhe2WlcnX0ZZNmNW2nZHnheIVlKGGveXzvbYQh[mW2YUSyJJBzd2S3Y4Tpc44hcW5iaIXtZY4hUDRiY3XscJMh\XiycnXzd4lv\yCqdX3hckBCWFBic4fl[Il{cCCvdYThcpQtKEmFNUC9NE4zOjVizszN NH;jO2IzOjR{MEi4OC=>
HEK293 cells MkG5SpVv[3Srb36gZZN{[Xl? M4DKdWlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIFjFT|I6OyClZXzsd{Bi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{NCCLQ{WwQVEvOiCwTR?= MonpNlM{OTJ7NES=
CHO cells MoT2SpVv[3Srb36gZZN{[Xl? MkjSTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHX4dJJme3OrbnegRXBRW3diYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjbYnsc4llKGKndHGoNUB1dyC6KTDz[YNz\XSrb36gZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhTUyLU1GsJGVFPTB;MT6yJI5O MoXRNlM4OTN4NU[=
human IMR32 cell NXLCfGhoTnWwY4Tpc44h[XO|YYm= M1jNWVIhcA>? MmW1TY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iaIXtZY4hUU2UM{KgZ4VtdCCvZX3idoFv\SC3c3nu[{BPd3SlaDDhd{B{fWK|dILheIUh[W[2ZYKgNkBpenNiYomgSWxKW0FuIFnDOVA:OS53IH7N MWKyN|MyOjl2NB?=
human 786-0 cell NFKzUGhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV3DcFV2UW6qaXLpeIlwdiCxZjDoeY1idiB5OE[tNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJzN{Og{txO M{LoPHNCVkeHUh?=
human NCI-H810 cell M3PwNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mo\UTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEixNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDJ3OUig{txO NGfxTHpUSU6JRWK=
human IGR-1 cell NXv0XZJPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3nUSGlvcGmkaYTpc44hd2ZiaIXtZY4hUUeULUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA1Pzd6IN88US=> MU\TRW5ITVJ?
human SK-MEL-3 cell NF;pblhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFTQXWdKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS52OUmyNkDPxE1? MnfJV2FPT0WU
human HT-1080 cell NHTZXoJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnm0TY5pcWKrdHnvckBw\iCqdX3hckBJXC1zMEiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk41QDd4NDFOwG0> NHHGPY5USU6JRWK=
human NCI-H23 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmHpTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46OzJ{IN88US=> NFLSW5JUSU6JRWK=
human Calu-6 cell NYDvRXRqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M37x[WlvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46PjBzNDFOwG0> NE\TOYVUSU6JRWK=
human CAPAN-1 cell MoT6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKGi3bXHuJGNCWEGQLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlE4QDh4IN88US=> NWDUTlN1W0GQR1XS
human COLO-668 cell Ml\pS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2Dnb2lvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22Olgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjRyMkKxJO69VQ>? MmL4V2FPT0WU
human TE-6 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWG3TFlOUW6qaXLpeIlwdiCxZjDoeY1idiCWRT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4yQTB6MjFOwG0> M1ntRnNCVkeHUh?=
human LCLC-97TM1 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVXJcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvOUfUUVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC5yOEi2JO69VQ>? MlqzV2FPT0WU
human CAS-1 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn3sTY5pcWKrdHnvckBw\iCqdX3hckBESVNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlY4OSEQvF2= MnjVV2FPT0WU
human RPMI-2650 cell NV3yNpB2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX\MOI83UW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVI3PTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz64NVI1KM7:TR?= NI\HO41USU6JRWK=
human MDA-MB-157 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2xOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC5{NEOxJO69VQ>? NGHXXHZUSU6JRWK=
human KINGS-1 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2TMdGlvcGmkaYTpc44hd2ZiaIXtZY4hU0mQR2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjN5NkKg{txO M3nPbnNCVkeHUh?=
human BB49-HNC cell NEPUblFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NILDfXRKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwNEGzPEDPxE1? M{W4WXNCVkeHUh?=
human SK-UT-1 cell M2XIPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkPGTY5pcWKrdHnvckBw\iCqdX3hckBUUy2XVD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPjh6MjFOwG0> NGHPSWZUSU6JRWK=
human EW-11 cell M2XodWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYPDVJh4UW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1Njh6M{Kg{txO NVvxc3dpW0GQR1XS
human D-502MG cell NXHpfGc2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYrJcohq[mm2aX;uJI9nKGi3bXHuJGQuPTB{TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE46ODN2IN88US=> NFv6OJlUSU6JRWK=
human MMAC-SF cell NV\CN|FmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn31TY5pcWKrdHnvckBw\iCqdX3hckBOVUGFLWPGJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvODh|MzFOwG0> MnqyV2FPT0WU
human NCI-H1648 cell NW\JUGhxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVHIRY5SUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNT63O|gh|ryP NWr6fIVSW0GQR1XS
human NCI-H292 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYPJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkmyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvQDhyNjFOwG0> NGnIR45USU6JRWK=
human NMC-G1 cell NWrnZotkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2ezO2lvcGmkaYTpc44hd2ZiaIXtZY4hVk2FLVexJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvPjJ7MzFOwG0> MnK1V2FPT0WU
human SAS cell MnnRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYfJcohq[mm2aX;uJI9nKGi3bXHuJHNCWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF5Lke4NVIh|ryP MnzsV2FPT0WU
human HCT-116 cell NEDIVFFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVzJcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPE44QTZ3IN88US=> MV7TRW5ITVJ?
human SBC-5 cell M{HLfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXiyRlVkUW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6NjB|IN88US=> MVrTRW5ITVJ?

... Click to View More Cell Line Experimental Data

体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[1]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 104 mg/mL (199.66 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 520.88
化学式

C20H17ClF4N4O4S

CAS号 1146699-66-2
储存条件 粉状
溶于溶剂
别名 N/A

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 ul 动物数量
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)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01002079 Completed Drug: BMS-708163|Drug: Rifampin Alzheimer Disease Bristol-Myers Squibb|PRA Health Sciences August 2010 Phase 1
NCT01057030 Completed Drug: BMS-708163|Drug: Placebo Alzheimer Disease Bristol-Myers Squibb March 2010 Phase 1
NCT01042314 Completed Drug: Donepezil|Drug: BMS-708163 Alzheimer Disease Bristol-Myers Squibb January 2010 Phase 1
NCT01039194 Completed Drug: galantamine|Drug: BMS-708163 Alzheimer Disease Bristol-Myers Squibb January 2010 Phase 1
NCT00979316 Completed Drug: BMS-708163|Drug: Placebo|Drug: Moxifloxacin Alzheimer Disease Bristol-Myers Squibb September 2009 Phase 1
NCT00890890 Terminated Drug: Avagacestat|Drug: Placebo Alzheimer''s Disease Bristol-Myers Squibb May 2009 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID