Avagacestat (BMS-708163)

Catalog No.S1262

For research use only.

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.

Avagacestat (BMS-708163) Chemical Structure

CAS No. 1146699-66-2

Selleck's Avagacestat (BMS-708163) has been cited by 21 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 M17z[2Z2dmO2aX;uJIF{e2G7 NYDoNm5MOiCq MmHJTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iaIXtZY4hUU2UM{KgZ4VtdCCvZX3idoFv\SC3c3nu[{BCWFBiYYOgd5Vje3S{YYTlJIFnfGW{IEKgbJJ{KGK7IFXMTXNCNCCLQ{WwQVAvOTNibl2= MYGyN|MyOjl2NB?=
human H4 cells Mki2SpVv[3Srb36gZZN{[Xl? M1Xv[mlvcGmkaYTpc44hd2ZiZ3HtcYEhe2WlcnX0ZZNmNW2nZHnheIVlKGGveXzvbYQh[mW2YUSyJJBzd2S3Y4Tpc44hcW5iaIXtZY4hUDRiY3XscJMh\XiycnXzd4lv\yCqdX3hckBCWFBic4fl[Il{cCCvdYThcpQtKEmFNUC9NE4zOjVizszN NEn0R|UzOjR{MEi4OC=>
HEK293 cells Mlq2SpVv[3Srb36gZZN{[Xl? NXfrbFR3UW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gTGVMOjl|IHPlcIx{KGGodHXyJI93\XKwaXfoeEBqdmO3YnH0bY9vKGK7IGfld5Rmem5iYnzveJRqdmdiYX7hcJl{cXNuIFnDOVA:OS5{IH7N NFn1SYYzOzNzMkm0OC=>
CHO cells Ml;lSpVv[3Srb36gZZN{[Xl? NHXwcWtKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCrbjDDTG8h[2WubIOgZZN{\XO|ZXSg[ZhxemW|c3nu[{BCWFCVdzDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHHtfYxwcWRiYnX0ZUgyKHSxIIipJJNm[3KndHnvckBi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCHTFnTRUwhTUR3ME2xMlIhdk1? MnPvNlM4OTN4NU[=
human IMR32 cell MnPlSpVv[3Srb36gZZN{[Xl? NF\QSXYzKGh? M3\MXGlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIHj1cYFvKEmPUkOyJINmdGxibXXtZpJidmVidYPpcochVm:2Y3igZZMhe3Wkc4TyZZRmKGGodHXyJFIhcHK|IHL5JGVNUVODLDDJR|UxRTFwNTDuUS=> M2K4e|I{OzF{OUS0
human 786-0 cell M{DBUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{\S[mlvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd|IN88US=> M{XuZ3NCVkeHUh?=
human NCI-H810 cell NVHJfZNHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{jLeWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi4NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR{NUm4JO69VQ>? NXHNfGdKW0GQR1XS
human IGR-1 cell M3TKOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmTjTY5pcWKrdHnvckBw\iCqdX3hckBKT1JvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFQ4PzhizszN MXPTRW5ITVJ?
human SK-MEL-3 cell MlLsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mm\LTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPDl7MkKg{txO MorPV2FPT0WU
human HT-1080 cell Mn3FS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEXVO5dKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUGwPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjR6N{[0JO69VQ>? NHfUWG1USU6JRWK=
human NCI-H23 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX31dJdTUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy57M{KyJO69VQ>? M{LHenNCVkeHUh?=
human Calu-6 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3\ZNmlvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46PjBzNDFOwG0> MoXiV2FPT0WU
human CAPAN-1 cell MlzOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGK3bnpKdmirYnn0bY9vKG:oIHj1cYFvKEODUFHOMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjF5OEi2JO69VQ>? MljRV2FPT0WU
human COLO-668 cell NWiwOphZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFrzXVdKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlY5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS52MEKyNUDPxE1? NIrJNW9USU6JRWK=
human TE-6 cell M1nxWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWX3bm5jUW6qaXLpeIlwdiCxZjDoeY1idiCWRT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4yQTB6MjFOwG0> NXrCd4I4W0GQR1XS
human LCLC-97TM1 cell M1GzZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfpTY5pcWKrdHnvckBw\iCqdX3hckBNS0yFLUm3WG0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTBwMEi4OkDPxE1? Ml[2V2FPT0WU
human CAS-1 cell M{fOTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVOxU4tJUW6qaXLpeIlwdiCxZjDoeY1idiCFQWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjZ5MTFOwG0> NEfMdpZUSU6JRWK=
human RPMI-2650 cell NUi1RZM4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkHETY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUK2OVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy56MUK0JO69VQ>? NYPib5JWW0GQR1XS
human MDA-MB-157 cell M4Lrbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX3YZnBxUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOTV5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuNlQ{OSEQvF2= MUXTRW5ITVJ?
human KINGS-1 cell NH\XOItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFPrZ|lKdmirYnn0bY9vKG:oIHj1cYFvKEuLTlfTMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC5|N{[yJO69VQ>? MojaV2FPT0WU
human BB49-HNC cell MnPuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPDF|ODFOwG0> NYW0VXVRW0GQR1XS
human SK-UT-1 cell M{XLVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXfJcohq[mm2aX;uJI9nKGi3bXHuJHNMNVWWLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE43QDh{IN88US=> Mn7yV2FPT0WU
human EW-11 cell MmLuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2P0PGlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE45QDN{IN88US=> M2q3eHNCVkeHUh?=
human D-502MG cell MljmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEPTN5pKdmirYnn0bY9vKG:oIHj1cYFvKERvNUCyUWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC57MEO0JO69VQ>? M{Txd3NCVkeHUh?=
human MMAC-SF cell M370Nmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX;Jcohq[mm2aX;uJI9nKGi3bXHuJG1OSUNvU1[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU4xQDN|IN88US=> MVXTRW5ITVJ?
human NCI-H1648 cell NITZTmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnrnTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS55N{ig{txO MlS4V2FPT0WU
human NCI-H292 cell MmPES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NY\Gd3FVUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF3Lki4NFYh|ryP NGLER5RUSU6JRWK=
human NMC-G1 cell NFLwZ5JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHTJdJBKdmirYnn0bY9vKG:oIHj1cYFvKE6PQz3HNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE3NjZ{OUOg{txO NWrQO3lnW0GQR1XS
human SAS cell NYf6fJJjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHNCWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF5Lke4NVIh|ryP NWDBd3lsW0GQR1XS
human HCT-116 cell MlHES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2WzTmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWLUGxOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE5Njd7NkWg{txO M{Wyd3NCVkeHUh?=
human SBC-5 cell NXKwRlZ1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYHJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuNFMh|ryP NF33bYhUSU6JRWK=
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 (from reference)

Animal Research:[1]
  • 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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 520.88
Formula

C20H17ClF4N4O4S

CAS No. 1146699-66-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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