Crenigacestat (LY3039478)

Catalog No.S7169

Crenigacestat (LY3039478) Chemical Structure

Molecular Weight(MW): 464.44

Crenigacestat (LY3039478) is an oral Notch inhibitor with an IC50 of 0.41 nM.

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Biological Activity

Description Crenigacestat (LY3039478) is an oral Notch inhibitor with an IC50 of 0.41 nM.
Targets
Notch-1 [1]
~1 nM
In vitro

LY3039478 is a novel small molecule that is an exquisitely potent inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with an IC50 of ∼1nM in most of the tumor cell lines tested. LY3039478 also potently inhibits mutant Notch receptor activity[2]. Treatment with a gamma secretase inhibitor, LY3039478, significantly inhibited the growth of 2 CCRCC(Clear cell renal cell carcinoma) cell lines in a concentration dependent manner. LY3039478 treatment also led to decreased expression of Myc and Cyclin A1, two genes that were part of the NOTCH driven proliferative signature in murine and human model systems. LY3039478 treatment also led to G0/G1 cell cycle arrest in CCRCC cells[3].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SW480 cells MX3GeY5kfGmxbjDhd5NigQ>? MUCyOEBp MXLJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKFOZNEiwJINmdGy|IHHzd4V{e2WmIHHzJI52[2ynYYKgZYNkfW23bHH0bY9vKG:oIF7veINpKDFiaX70doFk\WyudXzhdkBld22jaX6gLG4yUUOGKTDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNUC9NE4xODBzIN88US=> NIjzPGkzPDlyME[3PC=>
HEL 92.1.7 cells NUe0bZZkTnWwY4Tpc44h[XO|YYm= NYDnSWZEOjRiaB?= MXLJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKEiHTDC5Nk4yNjdiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1yLkCwNFI{KM7:TR?= MWWyOFkxODZ5OB?=
U-87-MG cells MYHGeY5kfGmxbjDhd5NigQ>? MYeyOEBp M{\NXWlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iVT24O{1OTyClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTBwMECwNlgh|ryP Moi3NlQ6ODB4N{i=
BxPC3 cells NFG3cWRHfW6ldHnvckBie3OjeR?= NEH2dZQzPCCq NX;JUXVoUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDCfHBEOyClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTBwMECwN|kh|ryP MlXoNlQ6ODB4N{i=
A375 cells MYrGeY5kfGmxbjDhd5NigQ>? M1ztRlI1KGh? NVXvVotXUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDBN|c2KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEC0PEDPxE1? M1S0OlI1QTByNke4
MDA-MB-231 Mmf5SpVv[3Srb36gZZN{[Xl? Mof6NlQhcA>? MUnJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1yLkCwNFUh|ryP NFzBV5AzPDlyME[3PC=>
MOLT-3 cells MYjGeY5kfGmxbjDhd5NigQ>? Mnr3NlQhcA>? NEj6RW1KdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIF3PUHQuOyClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTBwMECwOlEh|ryP NFTUVnQzPDlyME[3PC=>
MIAPaCa2 cells NX34dmF2TnWwY4Tpc44h[XO|YYm= MUeyOEBp M{nnW2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iTVnBVIFE[TJiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1yLkCwNFcyKM7:TR?= NHPZPJYzPDlyME[3PC=>
HCT 116 cells Mk\LSpVv[3Srb36gZZN{[Xl? NH\1ZoMzPCCq NHfHPY1KdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFjDWEAyOTZiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1yLkCwNFczKM7:TR?= MlLDNlQ6ODB4N{i=
K562 cells NVyz[nQ6TnWwY4Tpc44h[XO|YYm= NEfnVYMzPCCq NUDBR2F2UW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDLOVYzKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEC3OEDPxE1? NGnnclMzPDlyME[3PC=>
CCRF-CEM cells NVGxSnNoTnWwY4Tpc44h[XO|YYm= NEP1SY8zPCCq M1LwTmlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iQ1PSSk1ETU1iY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1yLkCwNFc3KM7:TR?= NYOzSot4OjR7MEC2O|g>
DLD1 cells MkfzSpVv[3Srb36gZZN{[Xl? MV:yOEBp MVfJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKESOREGgZ4VtdHNiYYPz[ZN{\WRiYYOgcpVkdGWjcjDhZ4N2dXWuYYTpc44hd2ZiTn;0Z4ghOSCrboTyZYNmdGy3bHHyJIRwdWGrbjCoUlFKS0RrIHHmeIVzKDJ2IHjyd{BjgSCHTFnTRUwhUUN3ME2wMlAxODl6IN88US=> M4X5eVI1QTByNke4
A2780 cells NX7mNlNSTnWwY4Tpc44h[XO|YYm= MoXPNlQhcA>? NFnNNXVKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFGyO|gxKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEGwN{DPxE1? MoPLNlQ6ODB4N{i=
SUP-T1 cells NHHSdlhHfW6ldHnvckBie3OjeR?= M{XCO|I1KGh? NYT2cFhCUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDTWXAuXDFiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1yLkCwNVI1KM7:TR?= NID4R3MzPDlyME[3PC=>
Jurkat cells NIj1XpBHfW6ldHnvckBie3OjeR?= M2SwSlI1KGh? NHe0XWtKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFr1dotifCClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTBwMEC1PVUh|ryP M1;F[lI1QTByNke4

... Click to View More Cell Line Experimental Data

In vivo In mice, its oral bioavalability(%F) is 65%, clearance(CL)=41 mL/min/kg, VDss = 3.8 L/kg. In Rats, its oral bioavalability(%F) is 65%, CL=98 mL/min/kg, VDss=4.9 L/kg. In Dogs, its oral bioavalability (%F) is 67%, CL=3.8 mL/min/kg, VDss=1.4 L/kg[1]. In a xenograft tumor model, LY3039478 inhibited N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment. The inhibition of Notch cleavage also resulted in the induction of apoptosis in a Notch-dependent xenograft model[2]. In immunodeficient NSG mice xenografted with 769-P CCRCC cells, LY3039478 treatment resulted in significantly increased survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC[3].

Protocol

Cell Research:

[4]

+ Expand
  • Cell lines: K07074 cells
  • Concentrations: 100 nM
  • Incubation Time: 24, 48, 72, 96 h
  • Method:

    K07074 cells were plated to 24-well plates at 105 cell/well. Viability of cells was assessed in quadruplicates at indicated timepoints using the CellTiter-Glo luminescent cell viability assay. To study the effect of the small molecular compounds on K07074 cell growth the compounds or DMSO were added to the growth media 24 h after seeding. The cells were incubated with inhibitors and DMSO as indicated. Cell viability was assessed as described above. Each experiment was carried out in triplicate and at least 3 independent experiments were performed.


    (Only for Reference)
Animal Research:

[3]

+ Expand
  • Animal Models: Mice
  • Formulation: 1% Na-CMC, 0.25% Tween-80 and 0.05% anti-foam
  • Dosages: 8 mg/kg
  • Administration: oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (198.08 mM)
Ethanol 71 mg/mL (152.87 mM)
Water 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 464.44
Formula

C22H23F3N4O4

CAS No. 1421438-81-4
Storage powder
in solvent
Synonyms

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID