Avagacestat (BMS-708163)

製品コードS1262

Avagacestat (BMS-708163)化学構造

分子量(MW):520.88

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.

サイズ 価格(税別)  
JPY 28220.00
JPY 53120.00
JPY 161020.00

カスタマーフィードバック(4)

  • A panel of GICs lines was treated with various concentrations of γ secretase inhibitors BMS-708163. Cells were treated with increasing concentrations of γ secretase inhibitors in triplicate wells for 72 hours, and cell viability was assessed by CellTiter-Blue assay as described in Materials and Methods. The results shown are of a single experiment with three independent replicates cell viability was measured by CellTiter-Blue assay. The graph depicts cell viability at 72 hours. Cell viability in the vehicle control was considered as to be 100%.

    Stem Cells 2014 32(1), 301-12. Avagacestat (BMS-708163) purchased from Selleck.

    Stem Cells 2014 32(1), 301-12. Avagacestat (BMS-708163) purchased from Selleck.

  • Aβ40 inhibition by γ-secretase inhibitors, DAPT and BMS-708163 (BMS). The amount of Aβ40 and Aβ42 in PS1-WT neurons treated with DMSO was defined as 1.0. *P < 0.05, as determined by Steel's test in comparison to PS1-G378E neurons treated with DMSO. Four independent experiments, each time in triplicates were performed (n = 4). Mean ± SD.

    Sci Rep, 2016, 6:33427. Avagacestat (BMS-708163) purchased from Selleck.

    Nuclear targeting of anMan-containing HS degradation products is suppressed by β-secretase inhibition in WT and Tg2576 MEFs and by γ-secretase inhibition in WT but not in Tg2576 MEFs. A-H, representative immunofluorescence images of wild-type MEF cells (A-D) and Tg2576 cells (E-H) treated with 100 nm β-inhibitor (A, B, E, and F) or 10 nM BMS-708163 (C, D, G, and H) for 48 h followed by treatment with 1 mm ascorbate for 1 h (B, D, F, and H) and then stained with DAPI and mAb AM. Bar, 20 um. Tg2576, MEFs from AD mouse model; DAPI, nuclear stain; Asc, ascorbate. These experiments were repeated twice.

    J Biol Chem 2014 289(30), 20871-8. Avagacestat (BMS-708163) purchased from Selleck.

製品安全説明書

Gamma-secretase阻害剤の選択性比較

生物活性

製品説明 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.
特性 Appears to be more “notch sparing” than semagacestat (LY450139).
ターゲット
γ secretase(Aβ42) [1]
(in H4-8Sw cells)
γ secretase(Aβ40) [1]
(in H4-8Sw cells)
0.27 nM 0.3 nM
体外試験

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

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human IMR32 cell MXvGeY5kfGmxbjDhd5NigQ>? NYP3OIZCOiCq NEXFboZKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCrbjDoeY1idiCLTWKzNkBk\WyuIH3lcYJz[W6nIIXzbY5oKEGSUDDhd{B{fWK|dILheIUh[W[2ZYKgNkBpenNiYomgSWxKW0FuIFnDOVA:OC5zMzDuUS=> NUWwVYd7OjN|MUK5OFQ>
human H4 cells NXi2b49RTnWwY4Tpc44h[XO|YYm= MVTJcohq[mm2aX;uJI9nKGejbX3hJJNm[3KndHHz[U1u\WSrYYTl[EBidXmub3nkJIJmfGF2MjDwdo9lfWO2aX;uJIlvKGi3bXHuJGg1KGOnbHzzJIV5eHKnc4PpcochcHWvYX6gRXBRKHO5ZXTpd4ghdXW2YX70MEBKSzVyPUCuNlI2KM7:TR?= MnHRNlI1OjB6OES=
HEK293 cells M4PQTWZ2dmO2aX;uJIF{e2G7 NU\RUppnUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gTGVMOjl|IHPlcIx{KGGodHXyJI93\XKwaXfoeEBqdmO3YnH0bY9vKGK7IGfld5Rmem5iYnzveJRqdmdiYX7hcJl{cXNuIFnDOVA:OS5{IH7N MmCzNlM{OTJ7NES=
CHO cells MVHGeY5kfGmxbjDhd5NigQ>? NUi4cYRDUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gR2hQKGOnbHzzJIF{e2W|c3XkJIV5eHKnc4PpcochSVCSU4egZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhcZltd2mmIHLleIEpOSC2bzD4LUB{\WO{ZYTpc44h[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nliRVzJV2EtKEWGNUC9NU4zKG6P NIK0bmQzOzdzM{[1Oi=>
human IMR32 cell NW[1OmdZTnWwY4Tpc44h[XO|YYm= NXrtOnFnOiCq NH2wbllKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCrbjDoeY1idiCLTWKzNkBk\WyuIH3lcYJz[W6nIIXzbY5oKE6xdHPoJIF{KHO3YoP0doF1\SCjZoTldkAzKGi{czDifUBGVEmVQTygTWM2OD1zLkWgcm0> NH;pfmgzOzNzMkm0OC=>
human 786-0 cell M4fZWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWjJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zNlE4OyEQvF2= M{HwSXNCVkeHUh?=
human NCI-H810 cell M2\Mdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KOEGwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OjV7ODFOwG0> MknmV2FPT0WU
human IGR-1 cell M1ziV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFLafo5KdmirYnn0bY9vKG:oIHj1cYFvKEmJUj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4xPDd5ODFOwG0> NXTHSm1sW0GQR1XS
human SK-MEL-3 cell NIPlNoxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF;qco9KdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS52OUmyNkDPxE1? MXjTRW5ITVJ?
human HT-1080 cell MmrOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoPZTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zMEiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk41QDd4NDFOwG0> NI[xZmhUSU6JRWK=
human NCI-H23 cell NHLqeZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWXJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk{OjJizszN MYPTRW5ITVJ?
human Calu-6 cell MmnmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXvJcohq[mm2aX;uJI9nKGi3bXHuJGNidHVvNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVYxOTRizszN NYDDfGFuW0GQR1XS
human CAPAN-1 cell NXf4c441T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXnjUG1jUW6qaXLpeIlwdiCxZjDoeY1idiCFQWDBUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5zN{i4OkDPxE1? MVjTRW5ITVJ?
human COLO-668 cell MmfoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWnnSIt6UW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY3QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNECyNlEh|ryP MlnYV2FPT0WU
human TE-6 cell NUHjN2NyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkG5NFgzKM7:TR?= M{jVS3NCVkeHUh?=
human LCLC-97TM1 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV\hSIxmUW6qaXLpeIlwdiCxZjDoeY1idiCOQ1zDMVk4XE1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNFg5PiEQvF2= M4LjdnNCVkeHUh?=
human CAS-1 cell NX34OnR{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXf1e2hzUW6qaXLpeIlwdiCxZjDoeY1idiCFQWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjZ5MTFOwG0> MlLoV2FPT0WU
human RPMI-2650 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MW\Jcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvMk[1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjhzMkSg{txO NVvaPI0xW0GQR1XS
human MDA-MB-157 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2xOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC5{NEOxJO69VQ>? MYHTRW5ITVJ?
human KINGS-1 cell MlPsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYTJcohq[mm2aX;uJI9nKGi3bXHuJGtKVkeVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE4{PzZ{IN88US=> NVLHcWxpW0GQR1XS
human BB49-HNC cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGrwd3lKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwNEGzPEDPxE1? NHru[XRUSU6JRWK=
human SK-UT-1 cell M3\KNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfTTY5pcWKrdHnvckBw\iCqdX3hckBUUy2XVD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPjh6MjFOwG0> MV;TRW5ITVJ?
human EW-11 cell NUTFfHRIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{jYPGlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE45QDN{IN88US=> MUHTRW5ITVJ?
human D-502MG cell MoLsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVHO[3VVUW6qaXLpeIlwdiCxZjDoeY1idiCGLUWwNm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwOUCzOEDPxE1? MUjTRW5ITVJ?
human MMAC-SF cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJG1OSUNvU1[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU4xQDN|IN88US=> NUnxcHBSW0GQR1XS
human NCI-H1648 cell NFzRNnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMU[0PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2Njd5ODFOwG0> M{jNN3NCVkeHUh?=
human NCI-H292 cell NH7GSVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnjwTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2Njh6ME[g{txO NU\wZYNrW0GQR1XS
human NMC-G1 cell M3nLPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlrOTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk43Ojl|IN88US=> MWnTRW5ITVJ?
human SAS cell NXzRWGxrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFK1PXFKdmirYnn0bY9vKG:oIHj1cYFvKFODUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG3Mlc5OTJizszN MVjTRW5ITVJ?
human HCT-116 cell MonHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV;ic2Q2UW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OThwN{m2OUDPxE1? M4Tre3NCVkeHUh?=
human SBC-5 cell NYi4VG5HT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlzBTY5pcWKrdHnvckBw\iCqdX3hckBUSkNvNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5MlA{KM7:TR?= NUj2V3g3W0GQR1XS

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

動物試験:[1]
+ 展開
  • 動物モデル: Female Harlan Sprague-Dawley rats or ATM-405-142K9 with 7- 10 month old Na?ve, grade II beagles
  • 製剤: 99% PEG-400, 1% Tween-80 (rats) or 94% labrafil-1944, 5% ethanol, 1% tween-80 (dogs)
  • 投薬量: 10 mg/kg (rats) or 2.5 mg/kg (dogs)
  • 投与方法: Dosed daily by oral gavage
    (参考用のみ)

溶解度 (25°C)

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

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 520.88
化学式

C20H17ClF4N4O4S

CAS No. 1146699-66-2
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01002079 Completed Alzheimer Disease Bristol-Myers Squibb|PRA Health Sciences August 2010 Phase 1
NCT01079819 Completed Alzheimer''s Disease Bristol-Myers Squibb April 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

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

Gamma-secretaseシグナル伝達経路

Gamma-secretase Inhibitors with Unique Features

相関Gamma-secretase製品

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID