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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Cited by 1 Publication

1 Customer Review

  • Effect of LY3039478 on Hes protein in SGC7901/DDP cells. A, Protein expression of Hes-1 by Western blot. B, Expression level of Hes-1 by Western blot experiment. (*p < 0.05 control with LY3039478 0 μmol/L group; **p < 0.01 control with LY3039478 0 μmol/L group).

    Eur Rev Med Pharmacol Sci, 2018, 22(13):4121-4127. Crenigacestat (LY3039478) purchased from Selleck.

Purity & Quality Control

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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 Mle3SpVv[3Srb36gZZN{[Xl? MnvtNlQhcA>? MY\Jcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKFOZNEiwJINmdGy|IHHzd4V{e2WmIHHzJI52[2ynYYKgZYNkfW23bHH0bY9vKG:oIF7veINpKDFiaX70doFk\WyudXzhdkBld22jaX6gLG4yUUOGKTDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNUC9NE4xODBzIN88US=> NV64dlZTOjR7MEC2O|g>
HEL 92.1.7 cells NXyxcnNnTnWwY4Tpc44h[XO|YYm= Ml3PNlQhcA>? MWPJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKEiHTDC5Nk4yNjdiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1yLkCwNFI{KM7:TR?= MlvGNlQ6ODB4N{i=
U-87-MG cells NVLmWplvTnWwY4Tpc44h[XO|YYm= NYC4XnhHOjRiaB?= NYrJNFF5UW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDVMVg4NU2JIHPlcIx{KGG|c3Xzd4VlKGG|IH71Z4xm[XJiYXPjeY12dGG2aX;uJI9nKE6xdHPoJFEhcW62cnHj[YxtfWyjcjDkc41icW5iKF6xTWNFMSCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTB;MD6wNFAzQCEQvF2= NXjiVG5ROjR7MEC2O|g>
BxPC3 cells NWr1Z2lNTnWwY4Tpc44h[XO|YYm= M{HRXlI1KGh? M{DkZWlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iQojQR|Mh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjByMEO5JO69VQ>? M1rLcVI1QTByNke4
A375 cells M1WxRWZ2dmO2aX;uJIF{e2G7 NGP5SFYzPCCq M3jkT2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iQUO3OUBk\WyuczDhd5Nme3OnZDDhd{BvfWOuZXHyJIFk[3WvdXzheIlwdiCxZjDOc5RkcCBzIHnueJJi[2WubIXsZZIh\G:vYXnuJEhPOUmFRDmgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwQVAvODByNEig{txO M{HKblI1QTByNke4
MDA-MB-231 MYrGeY5kfGmxbjDhd5NigQ>? NEOzfG4zPCCq M1PhWGlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjc4Pld5Nm\CCjczDueYNt\WG{IHHjZ5VufWyjdHnvckBw\iCQb4TjbEAyKGmwdILhZ4VtdHWuYYKg[I9u[WmwIDjONWlETCliYX\0[ZIhOjRiaILzJIJ6KEWOSWPBMEBKSzVyPUCuNFAxPSEQvF2= MoK1NlQ6ODB4N{i=
MOLT-3 cells Moj1SpVv[3Srb36gZZN{[Xl? MUKyOEBp MlnXTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCPT1zUMVMh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjByME[xJO69VQ>? M2fzfVI1QTByNke4
MIAPaCa2 cells NYDxPWduTnWwY4Tpc44h[XO|YYm= MYGyOEBp MWjJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKE2LQWDhR4EzKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEC3NUDPxE1? MmH4NlQ6ODB4N{i=
HCT 116 cells M2TScGZ2dmO2aX;uJIF{e2G7 NIfWXG4zPCCq NXrwU4RMUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDIR3QhOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IH71Z4xm[XJiYXPjeY12dGG2aX;uJI9nKE6xdHPoJFEhcW62cnHj[YxtfWyjcjDkc41icW5iKF6xTWNFMSCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTB;MD6wNFA4OiEQvF2= MUKyOFkxODZ5OB?=
K562 cells NUTvSHNSTnWwY4Tpc44h[XO|YYm= M{m3SlI1KGh? NIT1eZNKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFu1OlIh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjByMEe0JO69VQ>? MWKyOFkxODZ5OB?=
CCRF-CEM cells NVnuZlBFTnWwY4Tpc44h[XO|YYm= M{ntS|I1KGh? NIT1WFRKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFPDVmYuS0WPIHPlcIx{KGG|c3Xzd4VlKGG|IH71Z4xm[XJiYXPjeY12dGG2aX;uJI9nKE6xdHPoJFEhcW62cnHj[YxtfWyjcjDkc41icW5iKF6xTWNFMSCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTB;MD6wNFA4PiEQvF2= NHHPOlMzPDlyME[3PC=>
DLD1 cells MY\GeY5kfGmxbjDhd5NigQ>? NFrTZlAzPCCq MlzuTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCGTFSxJINmdGy|IHHzd4V{e2WmIHHzJI52[2ynYYKgZYNkfW23bHH0bY9vKG:oIF7veINpKDFiaX70doFk\WyudXzhdkBld22jaX6gLG4yUUOGKTDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNUC9NE4xODB7ODFOwG0> M3\vcFI1QTByNke4
A2780 cells NHKwOFhHfW6ldHnvckBie3OjeR?= NEPpOI4zPCCq NEXTe|FKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFGyO|gxKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEGwN{DPxE1? M13OW|I1QTByNke4
SUP-T1 cells Ml:xSpVv[3Srb36gZZN{[Xl? M{DzUFI1KGh? M1fE[mlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iU2XQMXQyKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEGyOEDPxE1? M4LnfVI1QTByNke4
Jurkat cells NEKybG5HfW6ldHnvckBie3OjeR?= Mn7PNlQhcA>? MmmyTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCMdYLrZZQh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjByNUm1JO69VQ>? M{P4flI1QTByNke4

... 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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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02906618 Completed Drug: LY3039478|Drug: 3C 15N 2H-LY3039478 IV Healthy Eli Lilly and Company October 4 2016 Phase 1
NCT02917733 Completed Drug: LY3039478 Healthy Eli Lilly and Company September 2016 Phase 1
NCT02836600 Active not recruiting Drug: LY3039478 Advanced Solid Tumor Eli Lilly and Company September 9 2016 Phase 1
NCT02518113 Completed Drug: LY3039478|Drug: Dexamethasone|Drug: Placebo T-cell Acute Lymphoblastic Leukemia|T-cell Lymphoblastic Lymphoma Eli Lilly and Company October 1 2015 Phase 1|Phase 2
NCT01695005 Completed Drug: LY3039478|Drug: Prednisone Neoplasms|Neoplasm Metastasis|Lymphoma Eli Lilly and Company October 2012 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID