Avagacestat (BMS-708163)

For research use only.

Catalog No.S1262

20 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.

Selleck's Avagacestat (BMS-708163) has been cited by 20 publications

Purity & Quality Control

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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 MoXZSpVv[3Srb36gZZN{[Xl? MV:yJIg> M2HZVmlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIHj1cYFvKEmPUkOyJINmdGxibXXtZpJidmVidYPpcochSVCSIHHzJJN2[nO2cnH0[UBi\nSncjCyJIhzeyCkeTDFUGlUSSxiSVO1NF0xNjF|IH7N NHn5cmszOzNzMkm0OC=>
human H4 cells MnjJSpVv[3Srb36gZZN{[Xl? M1\oVmlvcGmkaYTpc44hd2ZiZ3HtcYEhe2WlcnX0ZZNmNW2nZHnheIVlKGGveXzvbYQh[mW2YUSyJJBzd2S3Y4Tpc44hcW5iaIXtZY4hUDRiY3XscJMh\XiycnXzd4lv\yCqdX3hckBCWFBic4fl[Il{cCCvdYThcpQtKEmFNUC9NE4zOjVizszN NUHXRok6OjJ2MkC4PFQ>
HEK293 cells NVvtdpF6TnWwY4Tpc44h[XO|YYm= MmX5TY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iSFXLNlk{KGOnbHzzJIFnfGW{IH;2[ZJvcWeqdDDpcoN2[mG2aX;uJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZMtKEmFNUC9NU4zKG6P NUTNSXB1OjN|MUK5OFQ>
CHO cells MVLGeY5kfGmxbjDhd5NigQ>? MVLJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiZYjwdoV{e2mwZzDBVHBUfyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGGveXzvbYQh[mW2YTixJJRwKHhrIIPlZ5JmfGmxbjDh[pRmeiCxdnXycolocHRiaX7jeYJifGmxbjDifUBGVEmVQTygSWQ2OD1zLkKgcm0> NWHVbmEyOjN5MUO2OVY>
human IMR32 cell M1m3dmZ2dmO2aX;uJIF{e2G7 NGTId3YzKGh? MVTJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCqdX3hckBKVVJ|MjDj[YxtKG2nbXLyZY5mKHW|aX7nJG5wfGOqIHHzJJN2[nO2cnH0[UBi\nSncjCyJIhzeyCkeTDFUGlUSSxiSVO1NF0yNjVibl2= M4XTZVI{OzF{OUS0
human 786-0 cell NWrkPVdFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnTTTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuN|IyPzNizszN NGjBbHBUSU6JRWK=
human NCI-H810 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MojrTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEixNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDJ3OUig{txO NEjodVlUSU6JRWK=
human IGR-1 cell NG[5eXZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVPJcohq[mm2aX;uJI9nKGi3bXHuJGlIWi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wOFc4QCEQvF2= MVLTRW5ITVJ?
human SK-MEL-3 cell M{\rS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4HLcGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjR7OUKyJO69VQ>? NHHsZotUSU6JRWK=
human HT-1080 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGrxXmVKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUGwPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjR6N{[0JO69VQ>? NG\weFhUSU6JRWK=
human NCI-H23 cell MlvWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXzJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk{OjJizszN MkDHV2FPT0WU
human Calu-6 cell NEWxZ3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoPaTY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3LU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlk3ODF2IN88US=> NV;0bnVOW0GQR1XS
human CAPAN-1 cell NF7KV5JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWjJcohq[mm2aX;uJI9nKGi3bXHuJGNCWEGQLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlE4QDh4IN88US=> NWr3ZXFlW0GQR1XS
human COLO-668 cell Mn:wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1jzdWlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22Olgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjRyMkKxJO69VQ>? NVTHd4FEW0GQR1XS
human TE-6 cell MkDjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkG5NFgzKM7:TR?= MljKV2FPT0WU
human LCLC-97TM1 cell MkOxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVLUNJN[UW6qaXLpeIlwdiCxZjDoeY1idiCOQ1zDMVk4XE1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNFg5PiEQvF2= NUXDdIhIW0GQR1XS
human CAS-1 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MomzTY5pcWKrdHnvckBw\iCqdX3hckBESVNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlY4OSEQvF2= M{\6[HNCVkeHUh?=
human RPMI-2650 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlrxTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUK2OVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy56MUK0JO69VQ>? NVLLVWk6W0GQR1XS
human MDA-MB-157 cell NWTyVWNwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn3ITY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwMkSzNUDPxE1? M3nGSXNCVkeHUh?=
human KINGS-1 cell M3rrc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3uxNGlvcGmkaYTpc44hd2ZiaIXtZY4hU0mQR2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjN5NkKg{txO NFfZdJhUSU6JRWK=
human BB49-HNC cell Ml;RS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVrJcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPDF|ODFOwG0> NUf3dWpnW0GQR1XS
human SK-UT-1 cell NGPHZVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJHNMNVWWLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE43QDh{IN88US=> Ml3vV2FPT0WU
human EW-11 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mnn3TY5pcWKrdHnvckBw\iCqdX3hckBGXy1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0Mlg5OzJizszN MY\TRW5ITVJ?
human D-502MG cell NEewPFBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYHuN29wUW6qaXLpeIlwdiCxZjDoeY1idiCGLUWwNm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwOUCzOEDPxE1? MmHRV2FPT0WU
human MMAC-SF cell NVX0Ro5yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2HQWmlvcGmkaYTpc44hd2ZiaIXtZY4hVU2DQz3TSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjB6M{Og{txO M{DTb3NCVkeHUh?=
human NCI-H1648 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUDJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMU[0PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2Njd5ODFOwG0> M2O1S3NCVkeHUh?=
human NCI-H292 cell NGrObZFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVXPdnlRUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF3Lki4NFYh|ryP M2OxbnNCVkeHUh?=
human NMC-G1 cell MmfkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmSyTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk43Ojl|IN88US=> Mnr1V2FPT0WU
human SAS cell M3\sPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKGi3bXHuJHNCWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF5Lke4NVIh|ryP NXjQT3V5W0GQR1XS
human HCT-116 cell NX3WW41KT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXXMe5loUW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OThwN{m2OUDPxE1? MV3TRW5ITVJ?
human SBC-5 cell MoToS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX;ofIZ{UW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6NjB|IN88US=> MXHTRW5ITVJ?

... 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