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

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  • 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.
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 NXPkOIZ7TnWwY4Tpc44h[XO|YYm= M2XpSFI1KGh? NVzH[ZNMUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDTW|Q5OCClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTBwMECwNUDPxE1? MUWyOFkxODZ5OB?=
HEL 92.1.7 cells NID2XJhHfW6ldHnvckBie3OjeR?= NGe0S4EzPCCq NGHLcmpKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFjFUEA6Oi5zLkegZ4VtdHNiYYPz[ZN{\WRiYYOgcpVkdGWjcjDhZ4N2dXWuYYTpc44hd2ZiTn;0Z4ghOSCrboTyZYNmdGy3bHHyJIRwdWGrbjCoUlFKS0RrIHHmeIVzKDJ2IHjyd{BjgSCHTFnTRUwhUUN3ME2wMlAxODJ|IN88US=> MY[yOFkxODZ5OB?=
U-87-MG cells NFLVRo9HfW6ldHnvckBie3OjeR?= NHqweHMzPCCq M3\rW2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iVT24O{1OTyClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTBwMECwNlgh|ryP MUiyOFkxODZ5OB?=
BxPC3 cells MYXGeY5kfGmxbjDhd5NigQ>? MXiyOEBp NG\YSpFKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFL4VGM{KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMECzPUDPxE1? MUiyOFkxODZ5OB?=
A375 cells MoTaSpVv[3Srb36gZZN{[Xl? MVWyOEBp M{fKRWlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iQUO3OUBk\WyuczDhd5Nme3OnZDDhd{BvfWOuZXHyJIFk[3WvdXzheIlwdiCxZjDOc5RkcCBzIHnueJJi[2WubIXsZZIh\G:vYXnuJEhPOUmFRDmgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwQVAvODByNEig{txO NFvE[|EzPDlyME[3PC=>
MDA-MB-231 NYrPellOTnWwY4Tpc44h[XO|YYm= MXWyOEBp MoPrTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG|c3Xzd4VlKGG|IH71Z4xm[XJiYXPjeY12dGG2aX;uJI9nKE6xdHPoJFEhcW62cnHj[YxtfWyjcjDkc41icW5iKF6xTWNFMSCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTB;MD6wNFA2KM7:TR?= MYWyOFkxODZ5OB?=
MOLT-3 cells NUnnTlhHTnWwY4Tpc44h[XO|YYm= MWSyOEBp M17rT2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iTV;MWE0{KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEC2NUDPxE1? MVmyOFkxODZ5OB?=
MIAPaCa2 cells NX20VGFmTnWwY4Tpc44h[XO|YYm= MmHuNlQhcA>? NULsOXBYUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDNTWFR[UOjMjDj[YxteyCjc4Pld5Nm\CCjczDueYNt\WG{IHHjZ5VufWyjdHnvckBw\iCQb4TjbEAyKGmwdILhZ4VtdHWuYYKg[I9u[WmwIDjONWlETCliYX\0[ZIhOjRiaILzJIJ6KEWOSWPBMEBKSzVyPUCuNFAxPzFizszN MmHqNlQ6ODB4N{i=
HCT 116 cells NGLrcYZHfW6ldHnvckBie3OjeR?= NEGwR|UzPCCq M2PCN2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iSFPUJFEyPiClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTBwMECwO|Ih|ryP NXnWNJlROjR7MEC2O|g>
K562 cells MkDlSpVv[3Srb36gZZN{[Xl? M{HLcFI1KGh? NYXmUpZCUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDLOVYzKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEC3OEDPxE1? NVv0NZl7OjR7MEC2O|g>
CCRF-CEM cells M3LYUmZ2dmO2aX;uJIF{e2G7 M{XDTFI1KGh? M{fEWmlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iQ1PSSk1ETU1iY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1yLkCwNFc3KM7:TR?= NXmx[4FVOjR7MEC2O|g>
DLD1 cells NILZOJZHfW6ldHnvckBie3OjeR?= MYqyOEBp NGPMS3pKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIFTMSFEh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjByMEm4JO69VQ>? M3LZOlI1QTByNke4
A2780 cells MVLGeY5kfGmxbjDhd5NigQ>? MlThNlQhcA>? M17ST2lvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjByMUCzJO69VQ>? MWSyOFkxODZ5OB?=
SUP-T1 cells MYfGeY5kfGmxbjDhd5NigQ>? MkW0NlQhcA>? NVj2b4I6UW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDTWXAuXDFiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1yLkCwNVI1KM7:TR?= Mn;ZNlQ6ODB4N{i=
Jurkat cells NIPnOYZHfW6ldHnvckBie3OjeR?= MnfsNlQhcA>? M{fBXmlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iSoXyb4F1KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEW5OUDPxE1? M17SUVI1QTByNke4

... 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].


Cell Research:


+ 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:


+ 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


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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03502577 Recruiting Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) May 23 2018 Phase 1
NCT03502577 Recruiting Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) May 23 2018 Phase 1
NCT02784795 Active not recruiting Solid Tumor|Breast Cancer|Colon Cancer|Cholangiocarcinoma|Soft Tissue Sarcoma Eli Lilly and Company November 4 2016 Phase 1
NCT02784795 Active not recruiting Solid Tumor|Breast Cancer|Colon Cancer|Cholangiocarcinoma|Soft Tissue Sarcoma Eli Lilly and Company November 4 2016 Phase 1
NCT02906618 Completed Healthy Eli Lilly and Company October 4 2016 Phase 1
NCT02906618 Completed Healthy Eli Lilly and Company October 4 2016 Phase 1

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Gamma-secretase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID