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

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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 MmTLSpVv[3Srb36gZZN{[Xl? MlziNkBp NH7veVJKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCrbjDoeY1idiCLTWKzNkBk\WyuIH3lcYJz[W6nIIXzbY5oKEGSUDDhd{B{fWK|dILheIUh[W[2ZYKgNkBpenNiYomgSWxKW0FuIFnDOVA:OC5zMzDuUS=> NIDWOG4zOzNzMkm0OC=>
human H4 cells NX\ZfIM5TnWwY4Tpc44h[XO|YYm= NGnSXJNKdmirYnn0bY9vKG:oIHfhcY1iKHOnY4LleIF{\S2vZXTpZZRm\CCjbYnsc4llKGKndHG0NkBxem:mdXP0bY9vKGmwIHj1cYFvKEh2IHPlcIx{KGW6cILld5NqdmdiaIXtZY4hSVCSIIP3[YRqe2hibYX0ZY51NCCLQ{WwQVAvOjJ3IN88US=> M{KxVlIzPDJyOEi0
HEK293 cells M4HsSGZ2dmO2aX;uJIF{e2G7 M2TvU2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIFjFT|I6OyClZXzsd{Bi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{NCCLQ{WwQVEvOiCwTR?= MnHoNlM{OTJ7NES=
CHO cells MWTGeY5kfGmxbjDhd5NigQ>? NEHHTnFKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCrbjDDTG8h[2WubIOgZZN{\XO|ZXSg[ZhxemW|c3nu[{BCWFCVdzDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHHtfYxwcWRiYnX0ZUgyKHSxIIipJJNm[3KndHnvckBi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCHTFnTRUwhTUR3ME2xMlIhdk1? NXzmd3RPOjN5MUO2OVY>
human IMR32 cell M4XwXmZ2dmO2aX;uJIF{e2G7 NIXCO48zKGh? MVrJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCqdX3hckBKVVJ|MjDj[YxtKG2nbXLyZY5mKHW|aX7nJG5wfGOqIHHzJJN2[nO2cnH0[UBi\nSncjCyJIhzeyCkeTDFUGlUSSxiSVO1NF0yNjVibl2= NYnseYt5OjN|MUK5OFQ>
human 786-0 cell NXrFTJY{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4n6VWlvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd|IN88US=> NX;Sepo1W0GQR1XS
human NCI-H810 cell NWO5VJE2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmrtTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEixNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPDJ3OUig{txO NULHSYZQW0GQR1XS
human IGR-1 cell Ml\CS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1O2VmlvcGmkaYTpc44hd2ZiaIXtZY4hUUeULUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA1Pzd6IN88US=> MnvZV2FPT0WU
human SK-MEL-3 cell M{Tzbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXnJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41QTl{MjFOwG0> NHzGSlBUSU6JRWK=
human HT-1080 cell MkPKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2HpV2lvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUC4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPDh5NkSg{txO MnS0V2FPT0WU
human NCI-H23 cell NWPo[lk3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkfLTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46OzJ{IN88US=> MVjTRW5ITVJ?
human Calu-6 cell NELhXJlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoG4TY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3LU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlk3ODF2IN88US=> MVXTRW5ITVJ?
human CAPAN-1 cell MoS4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH22XIlKdmirYnn0bY9vKG:oIHj1cYFvKEODUFHOMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjF5OEi2JO69VQ>? MWrTRW5ITVJ?
human COLO-668 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mk\5TY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[2PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPDB{MkGg{txO NIrmOXRUSU6JRWK=
human TE-6 cell NH\nfVVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEnieIRKdmirYnn0bY9vKG:oIHj1cYFvKFSHLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlE6ODh{IN88US=> NIDqXnVUSU6JRWK=
human LCLC-97TM1 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVnCe5o1UW6qaXLpeIlwdiCxZjDoeY1idiCOQ1zDMVk4XE1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNFg5PiEQvF2= MkD0V2FPT0WU
human CAS-1 cell NUju[2ZsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWPJcohq[mm2aX;uJI9nKGi3bXHuJGNCWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOlcyKM7:TR?= NUDaXXp[W0GQR1XS
human RPMI-2650 cell NUTJbVR2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWrJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvMk[1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjhzMkSg{txO MlPVV2FPT0WU
human MDA-MB-157 cell NVOxTZRkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2H4SmlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVE2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2LkK0N|Eh|ryP NFnYVJpUSU6JRWK=
human KINGS-1 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmnZTY5pcWKrdHnvckBw\iCqdX3hckBMUU6JUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvOzd4MjFOwG0> NIi0U2NUSU6JRWK=
human BB49-HNC cell M{fE[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml:1TY5pcWKrdHnvckBw\iCqdX3hckBDSjR7LVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjRzM{ig{txO MYjTRW5ITVJ?
human SK-UT-1 cell NGnLdGVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKGi3bXHuJHNMNVWWLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE43QDh{IN88US=> NWLjUGxnW0GQR1XS
human EW-11 cell NVvnUoRnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWTm[2g{UW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1Njh6M{Kg{txO MYrTRW5ITVJ?
human D-502MG cell NXzhO4dKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUm3WoFvUW6qaXLpeIlwdiCxZjDoeY1idiCGLUWwNm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwOUCzOEDPxE1? NV[1doNrW0GQR1XS
human MMAC-SF cell NH;UcY1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJG1OSUNvU1[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU4xQDN|IN88US=> NVHMUG1HW0GQR1XS
human NCI-H1648 cell NYqxdVl4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYrRcFNPUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNT63O|gh|ryP M2\hTnNCVkeHUh?=
human NCI-H292 cell M1S5[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3[4eWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS56OEC2JO69VQ>? MnTVV2FPT0WU
human NMC-G1 cell MkHTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmW5TY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk43Ojl|IN88US=> MYDTRW5ITVJ?
human SAS cell Mn3jS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{DwdGlvcGmkaYTpc44hd2ZiaIXtZY4hW0GVIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUeuO|gyOiEQvF2= MXvTRW5ITVJ?
human HCT-116 cell NFT1eW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWfJcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPE44QTZ3IN88US=> MXjTRW5ITVJ?
human SBC-5 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuNFMh|ryP NULEZWtPW0GQR1XS

... 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