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 NEHwZXVHfW6ldHnvckBie3OjeR?= NYPVeWRvOiCq NY\ZZ2hIUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gbJVu[W5iSV3SN|Ih[2WubDDt[Y1jemGwZTD1d4lv\yCDUGCgZZMhe3Wkc4TyZZRmKGGodHXyJFIhcHK|IHL5JGVNUVODLDDJR|UxRTBwMUOgcm0> NVTCZZVPOjN|MUK5OFQ>
human H4 cells NILaZlRHfW6ldHnvckBie3OjeR?= Ml3rTY5pcWKrdHnvckBw\iCpYX3tZUB{\WO{ZYThd4UudWWmaXH0[YQh[W27bH;p[EBj\XSjNEKgdJJw\HWldHnvckBqdiCqdX3hckBJPCClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJGFRWCC|d3XkbZNpKG23dHHueEwhUUN3ME2wMlIzPSEQvF2= NGHt[FEzOjR{MEi4OC=>
HEK293 cells Mnn0SpVv[3Srb36gZZN{[Xl? MVrJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCKRVuyPVMh[2WubIOgZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpd{whUUN3ME2xMlIhdk1? NGTpeZMzOzNzMkm0OC=>
CHO cells NYfQdW06TnWwY4Tpc44h[XO|YYm= NYGwTHVrUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gR2hQKGOnbHzzJIF{e2W|c3XkJIV5eHKnc4PpcochSVCSU4egZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhcZltd2mmIHLleIEpOSC2bzD4LUB{\WO{ZYTpc44h[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nliRVzJV2EtKEWGNUC9NU4zKG6P NHGzSJkzOzdzM{[1Oi=>
human IMR32 cell MlWwSpVv[3Srb36gZZN{[Xl? M2DSdlIhcA>? M{DLV2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIHj1cYFvKEmPUkOyJINmdGxibXXtZpJidmVidYPpcochVm:2Y3igZZMhe3Wkc4TyZZRmKGGodHXyJFIhcHK|IHL5JGVNUVODLDDJR|UxRTFwNTDuUS=> NUTpXXM5OjN|MUK5OFQ>
human 786-0 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3nkNWlvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd|IN88US=> M1;6[HNCVkeHUh?=
human NCI-H810 cell NVy1N|Z1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn\3TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEixNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDJ3OUig{txO MVfTRW5ITVJ?
human IGR-1 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHjDboVKdmirYnn0bY9vKG:oIHj1cYFvKEmJUj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4xPDd5ODFOwG0> NF3uOZBUSU6JRWK=
human SK-MEL-3 cell M2\QPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41QTl{MjFOwG0> NHTNNI1USU6JRWK=
human HT-1080 cell MlvhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{jXdGlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUC4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPDh5NkSg{txO NEjwRWpUSU6JRWK=
human NCI-H23 cell NIm3cpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFvYR|JKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njl|MkKg{txO M3XV[nNCVkeHUh?=
human Calu-6 cell NGe4SHhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUH2OlRRUW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njl4MEG0JO69VQ>? MV3TRW5ITVJ?
human CAPAN-1 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXjzdWRPUW6qaXLpeIlwdiCxZjDoeY1idiCFQWDBUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5zN{i4OkDPxE1? M2faSXNCVkeHUh?=
human COLO-668 cell M1PWRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYfJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNk[4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41ODJ{MTFOwG0> M4\2UnNCVkeHUh?=
human TE-6 cell MnfsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MofYTY5pcWKrdHnvckBw\iCqdX3hckBVTS14IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj6xPVA5OiEQvF2= MYnTRW5ITVJ?
human LCLC-97TM1 cell MnvUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NED1[5hKdmirYnn0bY9vKG:oIHj1cYFvKEyFTFOtPVdVVTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMD6wPFg3KM7:TR?= NIHiV25USU6JRWK=
human CAS-1 cell NYPJT4dFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYPTTo9VUW6qaXLpeIlwdiCxZjDoeY1idiCFQWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjZ5MTFOwG0> NIHDSlFUSU6JRWK=
human RPMI-2650 cell NFTETI1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvMk[1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjhzMkSg{txO MWnTRW5ITVJ?
human MDA-MB-157 cell M3fvN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkXqTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwMkSzNUDPxE1? NVLG[5ZSW0GQR1XS
human KINGS-1 cell NVPSO41jT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmrLTY5pcWKrdHnvckBw\iCqdX3hckBMUU6JUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvOzd4MjFOwG0> NIL4UINUSU6JRWK=
human BB49-HNC cell NFzVb29Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYLJcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPDF|ODFOwG0> Ml7PV2FPT0WU
human SK-UT-1 cell NYDEUmN3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnrWYpKdmirYnn0bY9vKG:oIHj1cYFvKFONLWXUMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC54OEiyJO69VQ>? MX7TRW5ITVJ?
human EW-11 cell MoX6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF2ySGlKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvQDh|MjFOwG0> MUjTRW5ITVJ?
human D-502MG cell NInoUo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF30d|NKdmirYnn0bY9vKG:oIHj1cYFvKERvNUCyUWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC57MEO0JO69VQ>? NIfseW5USU6JRWK=
human MMAC-SF cell Ml;hS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX7Jcohq[mm2aX;uJI9nKGi3bXHuJG1OSUNvU1[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU4xQDN|IN88US=> MnjQV2FPT0WU
human NCI-H1648 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2fneWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlQ5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTVwN{e4JO69VQ>? MUDTRW5ITVJ?
human NCI-H292 cell M1WwVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NW\xc|Y2UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF3Lki4NFYh|ryP NYnLS4pyW0GQR1XS
human NMC-G1 cell NIXY[mdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUnJcohq[mm2aX;uJI9nKGi3bXHuJG5OSy2JMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG2MlYzQTNizszN NX\4ZWtYW0GQR1XS
human SAS cell M3G2dGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHHQTYJKdmirYnn0bY9vKG:oIHj1cYFvKFODUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG3Mlc5OTJizszN MknwV2FPT0WU
human HCT-116 cell MoXBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVjpS4R7UW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OThwN{m2OUDPxE1? MmXTV2FPT0WU
human SBC-5 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkDPTY5pcWKrdHnvckBw\iCqdX3hckBUSkNvNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5MlA{KM7:TR?= NVP2cmdCW0GQR1XS

... 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