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.

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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 M1\xZWZ2dmO2aX;uJIF{e2G7 M2C1dFIhcA>? MWnJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCqdX3hckBKVVJ|MjDj[YxtKG2nbXLyZY5mKHW|aX7nJGFRWCCjczDzeYJ{fHKjdHWgZYZ1\XJiMjDodpMh[nliRVzJV2EtKEmFNUC9NE4yOyCwTR?= M1j0U|I{OzF{OUS0
human H4 cells NWjtO4NwTnWwY4Tpc44h[XO|YYm= M{\qN2lvcGmkaYTpc44hd2ZiZ3HtcYEhe2WlcnX0ZZNmNW2nZHnheIVlKGGveXzvbYQh[mW2YUSyJJBzd2S3Y4Tpc44hcW5iaIXtZY4hUDRiY3XscJMh\XiycnXzd4lv\yCqdX3hckBCWFBic4fl[Il{cCCvdYThcpQtKEmFNUC9NE4zOjVizszN MXeyNlQzODh6NB?=
HEK293 cells MmnmSpVv[3Srb36gZZN{[Xl? M4Lhe2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIFjFT|I6OyClZXzsd{Bi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{NCCLQ{WwQVEvOiCwTR?= M3m4V|I{OzF{OUS0
CHO cells M1rMS2Z2dmO2aX;uJIF{e2G7 MVLJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiZYjwdoV{e2mwZzDBVHBUfyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGGveXzvbYQh[mW2YTixJJRwKHhrIIPlZ5JmfGmxbjDh[pRmeiCxdnXycolocHRiaX7jeYJifGmxbjDifUBGVEmVQTygSWQ2OD1zLkKgcm0> MYOyN|cyOzZ3Nh?=
human IMR32 cell M4jjdmZ2dmO2aX;uJIF{e2G7 NYS4bHZYOiCq NV7VXmRuUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gbJVu[W5iSV3SN|Ih[2WubDDt[Y1jemGwZTD1d4lv\yCQb4TjbEBieyC|dXLzeJJifGViYX\0[ZIhOiCqcoOgZpkhTUyLU1GsJGlEPTB;MT61JI5O NUTwdpM2OjN|MUK5OFQ>
human 786-0 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zNlE4OyEQvF2= Ml;qV2FPT0WU
human NCI-H810 cell MlLOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmrETY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEixNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDJ3OUig{txO Ml\kV2FPT0WU
human IGR-1 cell NWK5R|hMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnnWTY5pcWKrdHnvckBw\iCqdX3hckBKT1JvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFQ4PzhizszN M1fkSHNCVkeHUh?=
human SK-MEL-3 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWT3W3kzUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEm5NlIh|ryP MVTTRW5ITVJ?
human HT-1080 cell MmXwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3\jWWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUC4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPDh5NkSg{txO MWPTRW5ITVJ?
human NCI-H23 cell M1W0PGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFvOfI1KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njl|MkKg{txO MmjjV2FPT0WU
human Calu-6 cell MlG0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml24TY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3LU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlk3ODF2IN88US=> NGmwPZhUSU6JRWK=
human CAPAN-1 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{LmWmlvcGmkaYTpc44hd2ZiaIXtZY4hS0GSQV6tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOTd6OE[g{txO NV;MOlBrW0GQR1XS
human COLO-668 cell M1vCdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Moq0TY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[2PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDB{MkGg{txO MYDTRW5ITVJ?
human TE-6 cell M2DCPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFfpeYVKdmirYnn0bY9vKG:oIHj1cYFvKFSHLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlE6ODh{IN88US=> NF\SXllUSU6JRWK=
human LCLC-97TM1 cell NXjve5d[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvOUfUUVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC5yOEi2JO69VQ>? NFjzboJUSU6JRWK=
human CAS-1 cell NYrQWG1VT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGNCWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOlcyKM7:TR?= NHTO[IdUSU6JRWK=
human RPMI-2650 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3;zUGlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST2yOlUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwOEGyOEDPxE1? MV;TRW5ITVJ?
human MDA-MB-157 cell MnfQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1G2dGlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVE2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2LkK0N|Eh|ryP NUTic2c5W0GQR1XS
human KINGS-1 cell NWTafHBXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlLBTY5pcWKrdHnvckBw\iCqdX3hckBMUU6JUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvOzd4MjFOwG0> NUP6cXlqW0GQR1XS
human BB49-HNC cell NFLQT|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIH5RZhKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwNEGzPEDPxE1? MorLV2FPT0WU
human SK-UT-1 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{PnNmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvVWStNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjZ6OEKg{txO M4X3PXNCVkeHUh?=
human EW-11 cell M1n5cGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUHaPIhsUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1Njh6M{Kg{txO M2roXHNCVkeHUh?=
human D-502MG cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUD5fZFsUW6qaXLpeIlwdiCxZjDoeY1idiCGLUWwNm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwOUCzOEDPxE1? NWDBcVJbW0GQR1XS
human MMAC-SF cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mle5TY5pcWKrdHnvckBw\iCqdX3hckBOVUGFLWPGJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvODh|MzFOwG0> MV3TRW5ITVJ?
human NCI-H1648 cell NWnudoZFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHTNPJpKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY1QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF3Lke3PEDPxE1? MXLTRW5ITVJ?
human NCI-H292 cell NUnycXNxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHXuUIFKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlkzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTVwOEiwOkDPxE1? MWLTRW5ITVJ?
human NMC-G1 cell NGftXIJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mk\6TY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk43Ojl|IN88US=> M{PI[nNCVkeHUh?=
human SAS cell NHHYSY1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV3xSlNzUW6qaXLpeIlwdiCxZjDoeY1idiCVQWOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xO{44QDF{IN88US=> MlHXV2FPT0WU
human HCT-116 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF7SNppKdmirYnn0bY9vKG:oIHj1cYFvKEiFVD2xNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yQC55OU[1JO69VQ>? MV;TRW5ITVJ?
human SBC-5 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYTJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuNFMh|ryP MUXTRW5ITVJ?

... 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
in solvent
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 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

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