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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Cited by 8 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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Choose Selective Gamma-secretase Inhibitors

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 MYXGeY5kfGmxbjDhd5NigQ>? M3nq[|IhcA>? MljFTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iaIXtZY4hUU2UM{KgZ4VtdCCvZX3idoFv\SC3c3nu[{BCWFBiYYOgd5Vje3S{YYTlJIFnfGW{IEKgbJJ{KGK7IFXMTXNCNCCLQ{WwQVAvOTNibl2= MUGyN|MyOjl2NB?=
human H4 cells NYL5O5VGTnWwY4Tpc44h[XO|YYm= MnHTTY5pcWKrdHnvckBw\iCpYX3tZUB{\WO{ZYThd4UudWWmaXH0[YQh[W27bH;p[EBj\XSjNEKgdJJw\HWldHnvckBqdiCqdX3hckBJPCClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJGFRWCC|d3XkbZNpKG23dHHueEwhUUN3ME2wMlIzPSEQvF2= MVOyNlQzODh6NB?=
HEK293 cells NHXC[lZHfW6ldHnvckBie3OjeR?= NG\0fWpKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCrbjDISWszQTNiY3XscJMh[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nliV3XzeIVzdiCkbH;0eIlv\yCjbnHsfZNqeyxiSVO1NF0yNjJibl2= Mn\QNlM{OTJ7NES=
CHO cells Mo[4SpVv[3Srb36gZZN{[Xl? MVfJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiZYjwdoV{e2mwZzDBVHBUfyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGGveXzvbYQh[mW2YTixJJRwKHhrIIPlZ5JmfGmxbjDh[pRmeiCxdnXycolocHRiaX7jeYJifGmxbjDifUBGVEmVQTygSWQ2OD1zLkKgcm0> NXHJNpI5OjN5MUO2OVY>
human IMR32 cell NUTWNmo{TnWwY4Tpc44h[XO|YYm= NVrlT|ViOiCq M4G2b2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIHj1cYFvKEmPUkOyJINmdGxibXXtZpJidmVidYPpcochVm:2Y3igZZMhe3Wkc4TyZZRmKGGodHXyJFIhcHK|IHL5JGVNUVODLDDJR|UxRTFwNTDuUS=> NHvlc5MzOzNzMkm0OC=>
human 786-0 cell NGGye4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1fM[GlvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd|IN88US=> NE\NSmhUSU6JRWK=
human NCI-H810 cell NVjHfGRiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NETKW4ZKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IPFExKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkW5PEDPxE1? MnrJV2FPT0WU
human IGR-1 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGf5OFRKdmirYnn0bY9vKG:oIHj1cYFvKEmJUj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4xPDd5ODFOwG0> MmTTV2FPT0WU
human SK-MEL-3 cell NUHSS2hwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYS5Z|FqUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEm5NlIh|ryP M3vtWHNCVkeHUh?=
human HT-1080 cell NXeydFRrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGhVNTFyOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlQ5PzZ2IN88US=> NGHUVXJUSU6JRWK=
human NCI-H23 cell MkLMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVXJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk{OjJizszN M4LTNnNCVkeHUh?=
human Calu-6 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4r4NmlvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46PjBzNDFOwG0> M2fPb3NCVkeHUh?=
human CAPAN-1 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlXpTY5pcWKrdHnvckBw\iCqdX3hckBESVCDTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4yPzh6NjFOwG0> NV3nNVVlW0GQR1XS
human COLO-668 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNk[4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41ODJ{MTFOwG0> NYjuZ5BUW0GQR1XS
human TE-6 cell NH\CO3lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3ryZWlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNVkxQDJizszN NXXmUWRwW0GQR1XS
human LCLC-97TM1 cell M4nJfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn3lTY5pcWKrdHnvckBw\iCqdX3hckBNS0yFLUm3WG0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTBwMEi4OkDPxE1? MX3TRW5ITVJ?
human CAS-1 cell NWP2eolXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXfJcohq[mm2aX;uJI9nKGi3bXHuJGNCWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOlcyKM7:TR?= MnfPV2FPT0WU
human RPMI-2650 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWHvcHhlUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVI3PTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz64NVI1KM7:TR?= Ml35V2FPT0WU
human MDA-MB-157 cell M4W2WGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX\P[3kyUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOTV5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuNlQ{OSEQvF2= NXi3W2VSW0GQR1XS
human KINGS-1 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKGi3bXHuJGtKVkeVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE4{PzZ{IN88US=> NFX0emxUSU6JRWK=
human BB49-HNC cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1T6ZmlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ2OT3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC52MUO4JO69VQ>? MU\TRW5ITVJ?
human SK-UT-1 cell M375V2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NG\a[oVKdmirYnn0bY9vKG:oIHj1cYFvKFONLWXUMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC54OEiyJO69VQ>? MojDV2FPT0WU
human EW-11 cell MoHNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGVYNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuPFg{OiEQvF2= NXv5SXV6W0GQR1XS
human D-502MG cell M1[0VWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFf2PJFKdmirYnn0bY9vKG:oIHj1cYFvKERvNUCyUWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC57MEO0JO69VQ>? MoPtV2FPT0WU
human MMAC-SF cell NW[0V2FIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3[5WWlvcGmkaYTpc44hd2ZiaIXtZY4hVU2DQz3TSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjB6M{Og{txO NF:4VY9USU6JRWK=
human NCI-H1648 cell M3\DSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmHUTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS55N{ig{txO MmHGV2FPT0WU
human NCI-H292 cell NYDHbWkyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW[1WYFmUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF3Lki4NFYh|ryP NX\1TYhMW0GQR1XS
human NMC-G1 cell NXHZTlhuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUDJSVZ5UW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi54MkmzJO69VQ>? MX;TRW5ITVJ?
human SAS cell NWTYNW9yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmjiTY5pcWKrdHnvckBw\iCqdX3hckBUSVNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNz63PFEzKM7:TR?= NFLoV3BUSU6JRWK=
human HCT-116 cell MkD2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXXKU|BQUW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OThwN{m2OUDPxE1? M{jCcHNCVkeHUh?=
human SBC-5 cell NY\CN3NST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mlq2TY5pcWKrdHnvckBw\iCqdX3hckBUSkNvNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5MlA{KM7:TR?= NHvoT45USU6JRWK=

... 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
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
NCT01079819 Completed Alzheimer''s Disease Bristol-Myers Squibb April 2010 Phase 1
NCT01057030 Completed Alzheimer Disease Bristol-Myers Squibb March 2010 Phase 1
NCT01057030 Completed Alzheimer Disease Bristol-Myers Squibb March 2010 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

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Gamma-secretase Signaling Pathway Map

Gamma-secretase Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID