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 7 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.

  • 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

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 NEHPWXpHfW6ldHnvckBie3OjeR?= NVvTPFc1OiCq M{DN[mlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIHj1cYFvKEmPUkOyJINmdGxibXXtZpJidmVidYPpcochSVCSIHHzJJN2[nO2cnH0[UBi\nSncjCyJIhzeyCkeTDFUGlUSSxiSVO1NF0xNjF|IH7N MVeyN|MyOjl2NB?=
human H4 cells MnjSSpVv[3Srb36gZZN{[Xl? NG\YWGhKdmirYnn0bY9vKG:oIHfhcY1iKHOnY4LleIF{\S2vZXTpZZRm\CCjbYnsc4llKGKndHG0NkBxem:mdXP0bY9vKGmwIHj1cYFvKEh2IHPlcIx{KGW6cILld5NqdmdiaIXtZY4hSVCSIIP3[YRqe2hibYX0ZY51NCCLQ{WwQVAvOjJ3IN88US=> NG[wUYozOjR{MEi4OC=>
HEK293 cells NXX1[JA2TnWwY4Tpc44h[XO|YYm= MV;Jcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCKRVuyPVMh[2WubIOgZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpd{whUUN3ME2xMlIhdk1? MmWzNlM{OTJ7NES=
CHO cells M{TVeGZ2dmO2aX;uJIF{e2G7 MoTWTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHX4dJJme3OrbnegRXBRW3diYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjbYnsc4llKGKndHGoNUB1dyC6KTDz[YNz\XSrb36gZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhTUyLU1GsJGVFPTB;MT6yJI5O MVGyN|cyOzZ3Nh?=
human IMR32 cell NF3zVmVHfW6ldHnvckBie3OjeR?= MnfvNkBp Ml;wTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iaIXtZY4hUU2UM{KgZ4VtdCCvZX3idoFv\SC3c3nu[{BPd3SlaDDhd{B{fWK|dILheIUh[W[2ZYKgNkBpenNiYomgSWxKW0FuIFnDOVA:OS53IH7N MUiyN|MyOjl2NB?=
human 786-0 cell M3XF[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2O1fmlvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlMzOTd|IN88US=> MXnTRW5ITVJ?
human NCI-H810 cell NV3jSXNPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGLFPHZKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IPFExKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkW5PEDPxE1? NXrEe3NTW0GQR1XS
human IGR-1 cell NUnPVpVsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2rYXGlvcGmkaYTpc44hd2ZiaIXtZY4hUUeULUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA1Pzd6IN88US=> NV7VOWVpW0GQR1XS
human SK-MEL-3 cell NHja[|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIPhcmlKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS52OUmyNkDPxE1? Mk\ZV2FPT0WU
human HT-1080 cell M165NGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWrJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTFyOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlQ5PzZ2IN88US=> NH3EcVlUSU6JRWK=
human NCI-H23 cell M330d2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV3Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk{OjJizszN M1LrSXNCVkeHUh?=
human Calu-6 cell MmKxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUTJcohq[mm2aX;uJI9nKGi3bXHuJGNidHVvNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuPVYxOTRizszN M1LHWHNCVkeHUh?=
human CAPAN-1 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWPJcohq[mm2aX;uJI9nKGi3bXHuJGNCWEGQLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlE4QDh4IN88US=> MWTTRW5ITVJ?
human COLO-668 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1PJZmlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22Olgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjRyMkKxJO69VQ>? MnTTV2FPT0WU
human TE-6 cell NETJcppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF\kUFBKdmirYnn0bY9vKG:oIHj1cYFvKFSHLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlE6ODh{IN88US=> MXvTRW5ITVJ?
human LCLC-97TM1 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVvxZ5FuUW6qaXLpeIlwdiCxZjDoeY1idiCOQ1zDMVk4XE1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNFg5PiEQvF2= MnTrV2FPT0WU
human CAS-1 cell NFnhXYRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkjFTY5pcWKrdHnvckBw\iCqdX3hckBESVNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlY4OSEQvF2= NIjucZhUSU6JRWK=
human RPMI-2650 cell MkDwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIC0VHVKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtNlY2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkixNlQh|ryP Mln3V2FPT0WU
human MDA-MB-157 cell NW\xW|VPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUTMT3R1UW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOTV5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuNlQ{OSEQvF2= M2\5ZXNCVkeHUh?=
human KINGS-1 cell M2fnZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUDJcohq[mm2aX;uJI9nKGi3bXHuJGtKVkeVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE4{PzZ{IN88US=> NF7tXYVUSU6JRWK=
human BB49-HNC cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkPDTY5pcWKrdHnvckBw\iCqdX3hckBDSjR7LVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjRzM{ig{txO MYLTRW5ITVJ?
human SK-UT-1 cell NIfVcphIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUTORnFZUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3VWE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwNki4NkDPxE1? Ml7KV2FPT0WU
human EW-11 cell NVzTcIxiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUPJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuPFg{OiEQvF2= M4CxWXNCVkeHUh?=
human D-502MG cell NH;BdG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoixTY5pcWKrdHnvckBw\iCqdX3hckBFNTVyMl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvQTB|NDFOwG0> Mnz0V2FPT0WU
human MMAC-SF cell NVzuWm51T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml3YTY5pcWKrdHnvckBw\iCqdX3hckBOVUGFLWPGJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvODh|MzFOwG0> MV\TRW5ITVJ?
human NCI-H1648 cell NWHH[VJsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NU\RR2dKUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNT63O|gh|ryP MXXTRW5ITVJ?
human NCI-H292 cell NE\rUWRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkmyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvQDhyNjFOwG0> Mn7wV2FPT0WU
human NMC-G1 cell NEDDVHdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJG5OSy2JMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG2MlYzQTNizszN MWDTRW5ITVJ?
human SAS cell NFP6RXRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFniRYRKdmirYnn0bY9vKG:oIHj1cYFvKFODUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG3Mlc5OTJizszN NX\hdW1mW0GQR1XS
human HCT-116 cell MorGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV\lc5JtUW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OThwN{m2OUDPxE1? NFfCcplUSU6JRWK=
human SBC-5 cell MlrzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuNFMh|ryP MVfTRW5ITVJ?

... 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

Tel: +1-832-582-8158 Ext:3

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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