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

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 NVf4c2Z1TnWwY4Tpc44h[XO|YYm= NV7IS2oyOiCq NIDsSoxKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCrbjDoeY1idiCLTWKzNkBk\WyuIH3lcYJz[W6nIIXzbY5oKEGSUDDhd{B{fWK|dILheIUh[W[2ZYKgNkBpenNiYomgSWxKW0FuIFnDOVA:OC5zMzDuUS=> MmfvNlM{OTJ7NES=
human H4 cells M4X0dWZ2dmO2aX;uJIF{e2G7 MnnOTY5pcWKrdHnvckBw\iCpYX3tZUB{\WO{ZYThd4UudWWmaXH0[YQh[W27bH;p[EBj\XSjNEKgdJJw\HWldHnvckBqdiCqdX3hckBJPCClZXzsd{BmgHC{ZYPzbY5oKGi3bXHuJGFRWCC|d3XkbZNpKG23dHHueEwhUUN3ME2wMlIzPSEQvF2= NUTzNldOOjJ2MkC4PFQ>
HEK293 cells NILyOo1HfW6ldHnvckBie3OjeR?= M4jXTGlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIFjFT|I6OyClZXzsd{Bi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{NCCLQ{WwQVEvOiCwTR?= MUKyN|MyOjl2NB?=
CHO cells NYSxUJNyTnWwY4Tpc44h[XO|YYm= MmSxTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHX4dJJme3OrbnegRXBRW3diYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjbYnsc4llKGKndHGoNUB1dyC6KTDz[YNz\XSrb36gZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhTUyLU1GsJGVFPTB;MT6yJI5O NFGzdG0zOzdzM{[1Oi=>
human IMR32 cell Mnm3SpVv[3Srb36gZZN{[Xl? NEHmUnAzKGh? NXjneIJGUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gbJVu[W5iSV3SN|Ih[2WubDDt[Y1jemGwZTD1d4lv\yCQb4TjbEBieyC|dXLzeJJifGViYX\0[ZIhOiCqcoOgZpkhTUyLU1GsJGlEPTB;MT61JI5O MnXJNlM{OTJ7NES=
human 786-0 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVjBRXVoUW6qaXLpeIlwdiCxZjDoeY1idiB5OE[tNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJzN{Og{txO NHyzZ3hUSU6JRWK=
human NCI-H810 cell M2\tUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGr2VmxKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IPFExKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkW5PEDPxE1? MmjxV2FPT0WU
human IGR-1 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUnJcohq[mm2aX;uJI9nKGi3bXHuJGlIWi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wOFc4QCEQvF2= MoC5V2FPT0WU
human SK-MEL-3 cell NWTkNVhFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYPwdXF[UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEm5NlIh|ryP M2jBXXNCVkeHUh?=
human HT-1080 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHrrXpJKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUGwPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjR6N{[0JO69VQ>? MoHDV2FPT0WU
human NCI-H23 cell M{\zWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2PQfWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTN{MjFOwG0> NWSxfFFnW0GQR1XS
human Calu-6 cell NGLXVGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYS5ZZRiUW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njl4MEG0JO69VQ>? MmPSV2FPT0WU
human CAPAN-1 cell NETuN4VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYrlSItJUW6qaXLpeIlwdiCxZjDoeY1idiCFQWDBUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5zN{i4OkDPxE1? MoX1V2FPT0WU
human COLO-668 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUHJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNk[4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41ODJ{MTFOwG0> MlTlV2FPT0WU
human TE-6 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXixdYhlUW6qaXLpeIlwdiCxZjDoeY1idiCWRT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4yQTB6MjFOwG0> MnXGV2FPT0WU
human LCLC-97TM1 cell NVrGdph7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWfzfpZFUW6qaXLpeIlwdiCxZjDoeY1idiCOQ1zDMVk4XE1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNFg5PiEQvF2= Mmn5V2FPT0WU
human CAS-1 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXHXNYhWUW6qaXLpeIlwdiCxZjDoeY1idiCFQWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjZ5MTFOwG0> NH72dphUSU6JRWK=
human RPMI-2650 cell NY\3TVlQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml:5TY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUK2OVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy56MUK0JO69VQ>? MkHSV2FPT0WU
human MDA-MB-157 cell NX;xPFRkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUXwN2dDUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOTV5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuNlQ{OSEQvF2= MYjTRW5ITVJ?
human KINGS-1 cell M4LNN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV;FWIs3UW6qaXLpeIlwdiCxZjDoeY1idiCNSV7HV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwM{e2NkDPxE1? NYDBSo5TW0GQR1XS
human BB49-HNC cell NEn6fVZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NITaUI1KdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwNEGzPEDPxE1? Ml64V2FPT0WU
human SK-UT-1 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoiyTY5pcWKrdHnvckBw\iCqdX3hckBUUy2XVD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPjh6MjFOwG0> NEfVSFlUSU6JRWK=
human EW-11 cell NY\ON3hET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWq3ephRUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1Njh6M{Kg{txO Ml7yV2FPT0WU
human D-502MG cell M4jvWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXTzb3F1UW6qaXLpeIlwdiCxZjDoeY1idiCGLUWwNm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwOUCzOEDPxE1? NWPKUXhVW0GQR1XS
human MMAC-SF cell NH;mPYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3XpXGlvcGmkaYTpc44hd2ZiaIXtZY4hVU2DQz3TSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjB6M{Og{txO MWLTRW5ITVJ?
human NCI-H1648 cell NFvCVGtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmnNTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS55N{ig{txO M2LS[HNCVkeHUh?=
human NCI-H292 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NULhPYZJUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF3Lki4NFYh|ryP NIPZUoFUSU6JRWK=
human NMC-G1 cell NXjOcpFrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVTlS444UW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi54MkmzJO69VQ>? M2m1V3NCVkeHUh?=
human SAS cell M2PVfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIHxc5JKdmirYnn0bY9vKG:oIHj1cYFvKFODUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG3Mlc5OTJizszN NUnZSos3W0GQR1XS
human HCT-116 cell NEGwOFVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUTwXmRtUW6qaXLpeIlwdiCxZjDoeY1idiCKQ2StNVE3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OThwN{m2OUDPxE1? MWHTRW5ITVJ?
human SBC-5 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmmxTY5pcWKrdHnvckBw\iCqdX3hckBUSkNvNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5MlA{KM7:TR?= MV;TRW5ITVJ?

... 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
NCT01079819 Completed Alzheimer''s Disease Bristol-Myers Squibb April 2010 Phase 1
NCT01039194 Completed Alzheimer Disease Bristol-Myers Squibb January 2010 Phase 1
NCT00890890 Terminated Alzheimer''s Disease Bristol-Myers Squibb May 2009 Phase 2
NCT00810147 Completed Alzheimer''s Disease Bristol-Myers Squibb February 2009 Phase 2
NCT01454115 Completed Alzheimer''s Disease Bristol-Myers Squibb June 2007 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.

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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