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 NVnoSYl7TnWwY4Tpc44h[XO|YYm= NVe1fWJrOiCq MVHJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBqdiCqdX3hckBKVVJ|MjDj[YxtKG2nbXLyZY5mKHW|aX7nJGFRWCCjczDzeYJ{fHKjdHWgZYZ1\XJiMjDodpMh[nliRVzJV2EtKEmFNUC9NE4yOyCwTR?= NFrqcpQzOzNzMkm0OC=>
human H4 cells MkDKSpVv[3Srb36gZZN{[Xl? NFX2O5lKdmirYnn0bY9vKG:oIHfhcY1iKHOnY4LleIF{\S2vZXTpZZRm\CCjbYnsc4llKGKndHG0NkBxem:mdXP0bY9vKGmwIHj1cYFvKEh2IHPlcIx{KGW6cILld5NqdmdiaIXtZY4hSVCSIIP3[YRqe2hibYX0ZY51NCCLQ{WwQVAvOjJ3IN88US=> NHHyNXozOjR{MEi4OC=>
HEK293 cells NUH2bI5sTnWwY4Tpc44h[XO|YYm= MkjKTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iSFXLNlk{KGOnbHzzJIFnfGW{IH;2[ZJvcWeqdDDpcoN2[mG2aX;uJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZMtKEmFNUC9NU4zKG6P NGriXFMzOzNzMkm0OC=>
CHO cells MnvCSpVv[3Srb36gZZN{[Xl? Ml3CTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHX4dJJme3OrbnegRXBRW3diYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjbYnsc4llKGKndHGoNUB1dyC6KTDz[YNz\XSrb36gZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhTUyLU1GsJGVFPTB;MT6yJI5O MofWNlM4OTN4NU[=
human IMR32 cell NIWzSGVHfW6ldHnvckBie3OjeR?= NYLrfGlTOiCq NIryXHJKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCrbjDoeY1idiCLTWKzNkBk\WyuIH3lcYJz[W6nIIXzbY5oKE6xdHPoJIF{KHO3YoP0doF1\SCjZoTldkAzKGi{czDifUBGVEmVQTygTWM2OD1zLkWgcm0> NWL5emhkOjN|MUK5OFQ>
human 786-0 cell MoOxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX2wfpVuUW6qaXLpeIlwdiCxZjDoeY1idiB5OE[tNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzJzN{Og{txO NFPsWJRUSU6JRWK=
human NCI-H810 cell MnPlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3rPUGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi4NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjR{NUm4JO69VQ>? MXTTRW5ITVJ?
human IGR-1 cell NX;RZWhkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX7j[pZjUW6qaXLpeIlwdiCxZjDoeY1idiCLR2KtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODR5N{ig{txO MX7TRW5ITVJ?
human SK-MEL-3 cell MmfaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41QTl{MjFOwG0> MkTZV2FPT0WU
human HT-1080 cell NXfIV3hzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYLvVWdkUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2xNFgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi52OEe2OEDPxE1? NXv3RXpCW0GQR1XS
human NCI-H23 cell NYTTWoIzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGXZcG1KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njl|MkKg{txO MV;TRW5ITVJ?
human Calu-6 cell M1nXS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3qzSWlvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46PjBzNDFOwG0> NYPGPFlqW0GQR1XS
human CAPAN-1 cell NUfBbIRpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MofHTY5pcWKrdHnvckBw\iCqdX3hckBESVCDTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4yPzh6NjFOwG0> MkHDV2FPT0WU
human COLO-668 cell MlOwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX;kNoV6UW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY3QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNECyNlEh|ryP M3fCT3NCVkeHUh?=
human TE-6 cell NVThRYxLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmSwTY5pcWKrdHnvckBw\iCqdX3hckBVTS14IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj6xPVA5OiEQvF2= NHfaW5dUSU6JRWK=
human LCLC-97TM1 cell NYLJXmc4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3LlRWlvcGmkaYTpc44hd2ZiaIXtZY4hVEOOQz25O3ROOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFyLkC4PFYh|ryP MUfTRW5ITVJ?
human CAS-1 cell NFvSeYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIPWR4FKdmirYnn0bY9vKG:oIHj1cYFvKEODUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvPjdzIN88US=> NGDXUmFUSU6JRWK=
human RPMI-2650 cell MoXoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4PkfGlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST2yOlUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwOEGyOEDPxE1? NXXZeldLW0GQR1XS
human MDA-MB-157 cell NGPkbWpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4rYb2lvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVE2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2LkK0N|Eh|ryP M{mw[3NCVkeHUh?=
human KINGS-1 cell M2PlWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYrO[mptUW6qaXLpeIlwdiCxZjDoeY1idiCNSV7HV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwM{e2NkDPxE1? M17kfnNCVkeHUh?=
human BB49-HNC cell M2fRNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHjDNnBKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwNEGzPEDPxE1? MU\TRW5ITVJ?
human SK-UT-1 cell MkPNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXTpeo83UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3VWE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTRwNki4NkDPxE1? Ml7zV2FPT0WU
human EW-11 cell M{TtdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVPQVoZ5UW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1Njh6M{Kg{txO MXjTRW5ITVJ?
human D-502MG cell NFPMRpNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4nrfmlvcGmkaYTpc44hd2ZiaIXtZY4hTC13MELNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjlyM{Sg{txO MVfTRW5ITVJ?
human MMAC-SF cell M1v3U2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHLY[nVKdmirYnn0bY9vKG:oIHj1cYFvKE2PQVOtV2Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS5yOEOzJO69VQ>? M4TOV3NCVkeHUh?=
human NCI-H1648 cell NV7oVIxoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYL6RWtKUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNT63O|gh|ryP NGDhUXpUSU6JRWK=
human NCI-H292 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlraTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2Njh6ME[g{txO M{DIPXNCVkeHUh?=
human NMC-G1 cell M1KyWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoPHTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk43Ojl|IN88US=> Mm\3V2FPT0WU
human SAS cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX7SbYJHUW6qaXLpeIlwdiCxZjDoeY1idiCVQWOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xO{44QDF{IN88US=> M1y5TnNCVkeHUh?=
human HCT-116 cell NVnEeYZIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUDJcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPE44QTZ3IN88US=> NELTdHBUSU6JRWK=
human SBC-5 cell NX7rV|FIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYnJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy13IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuNFMh|ryP MlrVV2FPT0WU

... 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

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