Avagacestat (BMS-708163)

For research use only.

Catalog No.S1262

18 publications

Avagacestat (BMS-708163) Chemical Structure

CAS No. 1146699-66-2

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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Selleck's Avagacestat (BMS-708163) has been cited by 18 publications

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.

  • 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.

  • 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.

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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 MkPSSpVv[3Srb36gZZN{[Xl? NEG5ZWMzKGh? NYTZOpkxUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gbJVu[W5iSV3SN|Ih[2WubDDt[Y1jemGwZTD1d4lv\yCDUGCgZZMhe3Wkc4TyZZRmKGGodHXyJFIhcHK|IHL5JGVNUVODLDDJR|UxRTBwMUOgcm0> MoLBNlM{OTJ7NES=
human H4 cells MVrGeY5kfGmxbjDhd5NigQ>? NFnWSlhKdmirYnn0bY9vKG:oIHfhcY1iKHOnY4LleIF{\S2vZXTpZZRm\CCjbYnsc4llKGKndHG0NkBxem:mdXP0bY9vKGmwIHj1cYFvKEh2IHPlcIx{KGW6cILld5NqdmdiaIXtZY4hSVCSIIP3[YRqe2hibYX0ZY51NCCLQ{WwQVAvOjJ3IN88US=> MofRNlI1OjB6OES=
HEK293 cells Ml33SpVv[3Srb36gZZN{[Xl? M1G2bGlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIFjFT|I6OyClZXzsd{Bi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{NCCLQ{WwQVEvOiCwTR?= MUCyN|MyOjl2NB?=
CHO cells NV3sZY83TnWwY4Tpc44h[XO|YYm= MlTRTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHX4dJJme3OrbnegRXBRW3diYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjbYnsc4llKGKndHGoNUB1dyC6KTDz[YNz\XSrb36gZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhTUyLU1GsJGVFPTB;MT6yJI5O MVOyN|cyOzZ3Nh?=
human IMR32 cell MWPGeY5kfGmxbjDhd5NigQ>? MmLyNkBp MWPJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCqdX3hckBKVVJ|MjDj[YxtKG2nbXLyZY5mKHW|aX7nJG5wfGOqIHHzJJN2[nO2cnH0[UBi\nSncjCyJIhzeyCkeTDFUGlUSSxiSVO1NF0yNjVibl2= M1XldFI{OzF{OUS0
human 786-0 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFrUdlNKdmirYnn0bY9vKG:oIHj1cYFvKDd6Nj2wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{OjF5MzFOwG0> NIrHblBUSU6JRWK=
human NCI-H810 cell M2nBWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NG\MWnpKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IPFExKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkW5PEDPxE1? NXiweW5jW0GQR1XS
human IGR-1 cell MlHRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVG5O2pmUW6qaXLpeIlwdiCxZjDoeY1idiCLR2KtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODR5N{ig{txO MUPTRW5ITVJ?
human SK-MEL-3 cell NXjVfIs3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVm5W3Y3UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEm5NlIh|ryP NH2yb|JUSU6JRWK=
human HT-1080 cell NEXqSnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{DrWGlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUC4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPDh5NkSg{txO NFGwUIVUSU6JRWK=
human NCI-H23 cell NInhVXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NETVUpVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njl|MkKg{txO NWLPfWh6W0GQR1XS
human Calu-6 cell M3HXcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnHoTY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3LU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlk3ODF2IN88US=> NWjk[I1yW0GQR1XS
human CAPAN-1 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXHIeJB{UW6qaXLpeIlwdiCxZjDoeY1idiCFQWDBUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5zN{i4OkDPxE1? NWfCW5R[W0GQR1XS
human COLO-668 cell NWr6XpF6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mnm5TY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[2PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDB{MkGg{txO M1nlbnNCVkeHUh?=
human TE-6 cell NF62fYZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkG5NFgzKM7:TR?= M1W0VXNCVkeHUh?=
human LCLC-97TM1 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXzJcohq[mm2aX;uJI9nKGi3bXHuJGxEVENvOUfUUVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC5yOEi2JO69VQ>? NYraW3ZUW0GQR1XS
human CAS-1 cell M2Lnc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGNCWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOlcyKM7:TR?= M3fIV3NCVkeHUh?=
human RPMI-2650 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIXaW4dKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtNlY2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkixNlQh|ryP MWHTRW5ITVJ?
human MDA-MB-157 cell NIPCSFlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXvJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2xOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC5{NEOxJO69VQ>? NEC5e3hUSU6JRWK=
human KINGS-1 cell MnHXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M33MdmlvcGmkaYTpc44hd2ZiaIXtZY4hU0mQR2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjN5NkKg{txO M{XJUXNCVkeHUh?=
human BB49-HNC cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHjrb3hKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwNEGzPEDPxE1? M2H6b3NCVkeHUh?=
human SK-UT-1 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIHvNXBKdmirYnn0bY9vKG:oIHj1cYFvKFONLWXUMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC54OEiyJO69VQ>? NV:4W5hpW0GQR1XS
human EW-11 cell MnPUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnGxTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0Mlg5OzJizszN NHzhSZBUSU6JRWK=
human D-502MG cell M1jkbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M13NZ2lvcGmkaYTpc44hd2ZiaIXtZY4hTC13MELNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjlyM{Sg{txO NWnqPZJRW0GQR1XS
human MMAC-SF cell M4fNXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHHNelBKdmirYnn0bY9vKG:oIHj1cYFvKE2PQVOtV2Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS5yOEOzJO69VQ>? M4LObnNCVkeHUh?=
human NCI-H1648 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4POR2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlQ5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTVwN{e4JO69VQ>? NIXiT3ZUSU6JRWK=
human NCI-H292 cell NV\TfVFpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml;nTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2Njh6ME[g{txO NFX2XXJUSU6JRWK=
human NMC-G1 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYXJcohq[mm2aX;uJI9nKGi3bXHuJG5OSy2JMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG2MlYzQTNizszN NXzMNXdLW0GQR1XS
human SAS cell M1;yR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXriSHp{UW6qaXLpeIlwdiCxZjDoeY1idiCVQWOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xO{44QDF{IN88US=> MmLSV2FPT0WU
human HCT-116 cell MmKzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX3m[JU{UW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OThwN{m2OUDPxE1? M{HwW3NCVkeHUh?=
human SBC-5 cell M3\FdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUjJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuNFMh|ryP MWjTRW5ITVJ?

... 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]
- Collapse
  • Animal Models: Female Harlan Sprague-Dawley rats or ATM-405-142K9 with 7- 10 month old Na?ve, grade II beagles
  • 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
Smiles C1=CC(=CC=C1S(=O)(=O)N(CC2=C(C=C(C=C2)C3=NOC=N3)F)C(CCC(F)(F)F)C(=O)N)Cl

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Clinical Trial Information

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