Avagacestat (BMS-708163)

Catalog No.S1262

Avagacestat (BMS-708163) Chemical Structure

Molecular Weight(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.

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4 Customer Reviews

  • 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.

Purity & Quality Control

Choose Selective Gamma-secretase Inhibitors

Biological Activity

Description 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.
Features Appears to be more “notch sparing” than semagacestat (LY450139).
Targets
γ secretase(Aβ42) [1]
(in H4-8Sw cells)
γ secretase(Aβ40) [1]
(in H4-8Sw cells)
0.27 nM 0.3 nM
In vitro

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human IMR32 cell M3LneGZ2dmO2aX;uJIF{e2G7 NUS3VHBzOiCq MoizTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iaIXtZY4hUU2UM{KgZ4VtdCCvZX3idoFv\SC3c3nu[{BCWFBiYYOgd5Vje3S{YYTlJIFnfGW{IEKgbJJ{KGK7IFXMTXNCNCCLQ{WwQVAvOTNibl2= NWfDWFhiOjN|MUK5OFQ>
human H4 cells M3XyZWZ2dmO2aX;uJIF{e2G7 MkXpTY5pcWKrdHnvckBw\iCpYX3tZUB{\WO{ZYThd4UudWWmaXH0[YQh[W27bH;p[EBj\XSjNEKgdJJw\HWldHnvckBqdiCqdX3hckBJPCClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJGFRWCC|d3XkbZNpKG23dHHueEwhUUN3ME2wMlIzPSEQvF2= MXmyNlQzODh6NB?=
HEK293 cells Ml3vSpVv[3Srb36gZZN{[Xl? NXeyd25OUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gTGVMOjl|IHPlcIx{KGGodHXyJI93\XKwaXfoeEBqdmO3YnH0bY9vKGK7IGfld5Rmem5iYnzveJRqdmdiYX7hcJl{cXNuIFnDOVA:OS5{IH7N MXmyN|MyOjl2NB?=
CHO cells MXvGeY5kfGmxbjDhd5NigQ>? NVniOnFKUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gR2hQKGOnbHzzJIF{e2W|c3XkJIV5eHKnc4PpcochSVCSU4egZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhcZltd2mmIHLleIEpOSC2bzD4LUB{\WO{ZYTpc44h[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nliRVzJV2EtKEWGNUC9NU4zKG6P MoTrNlM4OTN4NU[=
human IMR32 cell NXrU[pJ4TnWwY4Tpc44h[XO|YYm= NG\Z[oUzKGh? MVvJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCqdX3hckBKVVJ|MjDj[YxtKG2nbXLyZY5mKHW|aX7nJG5wfGOqIHHzJJN2[nO2cnH0[UBi\nSncjCyJIhzeyCkeTDFUGlUSSxiSVO1NF0yNjVibl2= M2jGUlI{OzF{OUS0
human 786-0 cell NXO3cmh5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4jmWGlvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd|IN88US=> NX3hO3l6W0GQR1XS
human NCI-H810 cell NWTBcYFtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KOEGwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41OjV7ODFOwG0> M3fIUXNCVkeHUh?=
human IGR-1 cell Mom4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkHSTY5pcWKrdHnvckBw\iCqdX3hckBKT1JvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFQ4PzhizszN MVPTRW5ITVJ?
human SK-MEL-3 cell NXnIeIxLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWjyelBpUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEm5NlIh|ryP NW\PcmxLW0GQR1XS
human HT-1080 cell NVzTfmM2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn\CTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zMEiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk41QDd4NDFOwG0> MkjLV2FPT0WU
human NCI-H23 cell MkjRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3fCZmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTN{MjFOwG0> MnHnV2FPT0WU
human Calu-6 cell MoDpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWnJcohq[mm2aX;uJI9nKGi3bXHuJGNidHVvNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVYxOTRizszN MmLnV2FPT0WU
human CAPAN-1 cell NWDtV3JVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEHWTJJKdmirYnn0bY9vKG:oIHj1cYFvKEODUFHOMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjF5OEi2JO69VQ>? M4HudHNCVkeHUh?=
human COLO-668 cell MnH2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXPJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNk[4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41ODJ{MTFOwG0> NVf3dZFbW0GQR1XS
human TE-6 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIWyU4JKdmirYnn0bY9vKG:oIHj1cYFvKFSHLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlE6ODh{IN88US=> NUXPVlNuW0GQR1XS
human LCLC-97TM1 cell M2TCWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUTJcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvOUfUUVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC5yOEi2JO69VQ>? M1LkOXNCVkeHUh?=
human CAS-1 cell M2DZN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1vtPWlvcGmkaYTpc44hd2ZiaIXtZY4hS0GVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{43PzFizszN MYrTRW5ITVJ?
human RPMI-2650 cell M1y4Smdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVHJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvMk[1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjhzMkSg{txO NFPxZYhUSU6JRWK=
human MDA-MB-157 cell M{XtdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoXNTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwMkSzNUDPxE1? MlvMV2FPT0WU
human KINGS-1 cell NGO2U29Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn7GTY5pcWKrdHnvckBw\iCqdX3hckBMUU6JUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvOzd4MjFOwG0> NV\5fpRjW0GQR1XS
human BB49-HNC cell MlzFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NU\me5lEUW6qaXLpeIlwdiCxZjDoeY1idiCEQkS5MWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2LkSxN|gh|ryP M3nGd3NCVkeHUh?=
human SK-UT-1 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mny3TY5pcWKrdHnvckBw\iCqdX3hckBUUy2XVD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPjh6MjFOwG0> NVTMTmdyW0GQR1XS
human EW-11 cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVzJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuPFg{OiEQvF2= MnjUV2FPT0WU
human D-502MG cell NUe1SIhYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKGi3bXHuJGQuPTB{TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE46ODN2IN88US=> Mn\oV2FPT0WU
human MMAC-SF cell NIrlXnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{jYe2lvcGmkaYTpc44hd2ZiaIXtZY4hVU2DQz3TSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjB6M{Og{txO NWfNcGxNW0GQR1XS
human NCI-H1648 cell NIDvfZBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlvVTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS55N{ig{txO NWDkSZc3W0GQR1XS
human NCI-H292 cell NFz1W5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIK5b5hKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlkzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTVwOEiwOkDPxE1? NYDodo91W0GQR1XS
human NMC-G1 cell NW\0PW1bT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoDWTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk43Ojl|IN88US=> M3L3PXNCVkeHUh?=
human SAS cell M1rxT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoHwTY5pcWKrdHnvckBw\iCqdX3hckBUSVNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNz63PFEzKM7:TR?= NVHqXmh{W0GQR1XS
human HCT-116 cell M{KzRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXXJcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPE44QTZ3IN88US=> NVzzToYzW0GQR1XS
human SBC-5 cell NXHPVYEyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWXo[YN1UW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6NjB|IN88US=> MmGzV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Female Harlan Sprague-Dawley rats or ATM-405-142K9 with 7- 10 month old Na?ve, grade II beagles
  • Formulation: 99% PEG-400, 1% Tween-80 (rats) or 94% labrafil-1944, 5% ethanol, 1% tween-80 (dogs)
  • Dosages: 10 mg/kg (rats) or 2.5 mg/kg (dogs)
  • Administration: Dosed daily by oral gavage
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 520.88
Formula

C20H17ClF4N4O4S

CAS No. 1146699-66-2
Storage powder
Synonyms N/A

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Clinical Trial Information

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 Alzheimers Disease Bristol-Myers Squibb April 2010 Phase 1
NCT01057030 Completed Alzheimer Disease Bristol-Myers Squibb March 2010 Phase 1
NCT01039194 Completed Alzheimer Disease Bristol-Myers Squibb January 2010 Phase 1
NCT01042314 Completed Alzheimer Disease Bristol-Myers Squibb January 2010 Phase 1
NCT00979316 Completed Alzheimer Disease Bristol-Myers Squibb September 2009 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Gamma-secretase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID