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.

Size Price Stock Quantity  
USD 170 In stock
USD 320 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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 M1nXSGZ2dmO2aX;uJIF{e2G7 NYDDPJZzOiCq MkPnTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iaIXtZY4hUU2UM{KgZ4VtdCCvZX3idoFv\SC3c3nu[{BCWFBiYYOgd5Vje3S{YYTlJIFnfGW{IEKgbJJ{KGK7IFXMTXNCNCCLQ{WwQVAvOTNibl2= MW[yN|MyOjl2NB?=
human H4 cells MXrGeY5kfGmxbjDhd5NigQ>? NVXhSVdMUW6qaXLpeIlwdiCxZjDnZY1u[SC|ZXPy[ZRie2VvbXXkbYF1\WRiYX35cI9q\CCkZYThOFIheHKxZIXjeIlwdiCrbjDoeY1idiCKNDDj[YxteyCneIDy[ZN{cW6pIHj1cYFvKEGSUDDze4VlcXOqIH31eIFvfCxiSVO1NF0xNjJ{NTFOwG0> M4rpS|IzPDJyOEi0
HEK293 cells NF;qVIJHfW6ldHnvckBie3OjeR?= M13LVWlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKGmwIFjFT|I6OyClZXzsd{Bi\nSncjDveoVzdmmpaISgbY5kfWKjdHnvckBjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{NCCLQ{WwQVEvOiCwTR?= MkXVNlM{OTJ7NES=
CHO cells MVzGeY5kfGmxbjDhd5NigQ>? NWqwPJk5UW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2ViaX6gR2hQKGOnbHzzJIF{e2W|c3XkJIV5eHKnc4PpcochSVCSU4egZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhcZltd2mmIHLleIEpOSC2bzD4LUB{\WO{ZYTpc44h[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nliRVzJV2EtKEWGNUC9NU4zKG6P MmS3NlM4OTN4NU[=
human IMR32 cell MUTGeY5kfGmxbjDhd5NigQ>? NX3tOVRIOiCq MnTKTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iaIXtZY4hUU2UM{KgZ4VtdCCvZX3idoFv\SC3c3nu[{BPd3SlaDDhd{B{fWK|dILheIUh[W[2ZYKgNkBpenNiYomgSWxKW0FuIFnDOVA:OS53IH7N MXWyN|MyOjl2NB?=
human 786-0 cell NEjsZ5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUTJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zNlE4OyEQvF2= MmnvV2FPT0WU
human NCI-H810 cell M3rucGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFrrb5ZKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IPFExKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MkW5PEDPxE1? NIrXcI9USU6JRWK=
human IGR-1 cell M1;6UWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3Sy[mlvcGmkaYTpc44hd2ZiaIXtZY4hUUeULUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA1Pzd6IN88US=> NWO3Zo04W0GQR1XS
human SK-MEL-3 cell NULXSHVbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41QTl{MjFOwG0> NHT1bG9USU6JRWK=
human HT-1080 cell NFvWOFJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHT6SZlKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUGwPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjR6N{[0JO69VQ>? MmTVV2FPT0WU
human NCI-H23 cell MknGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3HVd2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTN{MjFOwG0> M1LoRXNCVkeHUh?=
human Calu-6 cell MmPIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVWze2RkUW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njl4MEG0JO69VQ>? NWHiSXNVW0GQR1XS
human CAPAN-1 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkDKTY5pcWKrdHnvckBw\iCqdX3hckBESVCDTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4yPzh6NjFOwG0> M3y5d3NCVkeHUh?=
human COLO-668 cell MormS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXrJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNk[4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41ODJ{MTFOwG0> M1v4SHNCVkeHUh?=
human TE-6 cell NHPwSGFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIDON|RKdmirYnn0bY9vKG:oIHj1cYFvKFSHLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlE6ODh{IN88US=> NH3GbG9USU6JRWK=
human LCLC-97TM1 cell Mk\hS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVu3do5yUW6qaXLpeIlwdiCxZjDoeY1idiCOQ1zDMVk4XE1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNFg5PiEQvF2= NETvT4pUSU6JRWK=
human CAS-1 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWC1TFJTUW6qaXLpeIlwdiCxZjDoeY1idiCFQWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE{NjZ5MTFOwG0> MnjhV2FPT0WU
human RPMI-2650 cell NWXzRVZPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH7adHBKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtNlY2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkixNlQh|ryP MXvTRW5ITVJ?
human MDA-MB-157 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkHJTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNVU4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwMkSzNUDPxE1? NVPWeZRyW0GQR1XS
human KINGS-1 cell M33pcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlX0TY5pcWKrdHnvckBw\iCqdX3hckBMUU6JUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvOzd4MjFOwG0> NGnPN|JUSU6JRWK=
human BB49-HNC cell NWP1XJRZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGXSN5VKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwNEGzPEDPxE1? MlHpV2FPT0WU
human SK-UT-1 cell M3W2fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfjTY5pcWKrdHnvckBw\iCqdX3hckBUUy2XVD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPjh6MjFOwG0> M1LWV3NCVkeHUh?=
human EW-11 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUPJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuPFg{OiEQvF2= NWTDW5FUW0GQR1XS
human D-502MG cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2PE[WlvcGmkaYTpc44hd2ZiaIXtZY4hTC13MELNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjlyM{Sg{txO NXLFTJRTW0GQR1XS
human MMAC-SF cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJG1OSUNvU1[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU4xQDN|IN88US=> NX\VOJdyW0GQR1XS
human NCI-H1648 cell MlnVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MljpTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS55N{ig{txO MoLFV2FPT0WU
human NCI-H292 cell MnSyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkmyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvQDhyNjFOwG0> MoL2V2FPT0WU
human NMC-G1 cell M3rEeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXP1TWJuUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPi54MkmzJO69VQ>? MVLTRW5ITVJ?
human SAS cell NUjuOWNST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmnxTY5pcWKrdHnvckBw\iCqdX3hckBUSVNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNz63PFEzKM7:TR?= Mn7CV2FPT0WU
human HCT-116 cell NVHlfG9TT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYXJcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPE44QTZ3IN88US=> MUXTRW5ITVJ?
human SBC-5 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1njeGlvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU4xOyEQvF2= MWfTRW5ITVJ?

... 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Gamma-secretase Signaling Pathway Map

Gamma-secretase Inhibitors with Unique Features

Related Gamma-secretase Products

Tags: buy Avagacestat (BMS-708163) | Avagacestat (BMS-708163) supplier | purchase Avagacestat (BMS-708163) | Avagacestat (BMS-708163) cost | Avagacestat (BMS-708163) manufacturer | order Avagacestat (BMS-708163) | Avagacestat (BMS-708163) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID