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 NILoWXlHfW6ldHnvckBie3OjeR?= MlfTNlQhcA>? MkHBTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCVV{S4NEBk\WyuczDhd5Nme3OnZDDhd{BvfWOuZXHyJIFk[3WvdXzheIlwdiCxZjDOc5RkcCBzIHnueJJi[2WubIXsZZIh\G:vYXnuJEhPOUmFRDmgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwQVAvODByMTFOwG0> MU[yOFkxODZ5OB?=
HEL 92.1.7 cells MX\GeY5kfGmxbjDhd5NigQ>? NUHsXnE2OjRiaB?= MmO2TY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCKRVygPVIvOS55IHPlcIx{KGG|c3Xzd4VlKGG|IH71Z4xm[XJiYXPjeY12dGG2aX;uJI9nKE6xdHPoJFEhcW62cnHj[YxtfWyjcjDkc41icW5iKF6xTWNFMSCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTB;MD6wNFAzOyEQvF2= MV2yOFkxODZ5OB?=
U-87-MG cells MWPGeY5kfGmxbjDhd5NigQ>? NG[yO3QzPCCq MYTJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKFVvOEetUWch[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjByMEK4JO69VQ>? Ml3TNlQ6ODB4N{i=
BxPC3 cells M3jacGZ2dmO2aX;uJIF{e2G7 MYqyOEBp NXi2ZnRoUW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDCfHBEOyClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTBwMECwN|kh|ryP NVzvNm15OjR7MEC2O|g>
A375 cells NVrtXm9zTnWwY4Tpc44h[XO|YYm= Mo[1NlQhcA>? M4XZSWlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iQUO3OUBk\WyuczDhd5Nme3OnZDDhd{BvfWOuZXHyJIFk[3WvdXzheIlwdiCxZjDOc5RkcCBzIHnueJJi[2WubIXsZZIh\G:vYXnuJEhPOUmFRDmgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwQVAvODByNEig{txO MmH3NlQ6ODB4N{i=
MDA-MB-231 NVu2d2xITnWwY4Tpc44h[XO|YYm= M4XCe|I1KGh? NV\BRVU4UW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHzd4V{e2WmIHHzJI52[2ynYYKgZYNkfW23bHH0bY9vKG:oIF7veINpKDFiaX70doFk\WyudXzhdkBld22jaX6gLG4yUUOGKTDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNUC9NE4xODB3IN88US=> M{L3[VI1QTByNke4
MOLT-3 cells MWnGeY5kfGmxbjDhd5NigQ>? M{nTbFI1KGh? MoTCTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCPT1zUMVMh[2WubIOgZZN{\XO|ZXSgZZMhdnWlbHXhdkBi[2O3bYXsZZRqd25ib3[gUo91[2hiMTDpcpRz[WOnbHz1cIFzKGSxbXHpckApVjGLQ1SpJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjByME[xJO69VQ>? NYe3RllUOjR7MEC2O|g>
MIAPaCa2 cells MofpSpVv[3Srb36gZZN{[Xl? MlLyNlQhcA>? M4r5TGlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iTVnBVIFE[TJiY3XscJMh[XO|ZYPz[YQh[XNiboXjcIVieiCjY3P1cZVt[XSrb36gc4YhVm:2Y3igNUBqdnS{YXPlcIx2dGG{IHTvcYFqdiBqTkHJR2QqKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1yLkCwNFcyKM7:TR?= NIDKVm4zPDlyME[3PC=>
HCT 116 cells M176UGZ2dmO2aX;uJIF{e2G7 M2n2XVI1KGh? MoXDTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCKQ2SgNVE3KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEC3NkDPxE1? MmH5NlQ6ODB4N{i=
K562 cells M4r4WGZ2dmO2aX;uJIF{e2G7 NUe0RVlEOjRiaB?= Mn;yTY5pcWKrdHnvckBw\iCpYX3tZU1{\WO{ZYThd4UhdWWmaXH0[YQh[2ynYY\h[4Uhd2ZiTn;0Z4ghOSCrbjDoeY1idiCNNU[yJINmdGy|IHHzd4V{e2WmIHHzJI52[2ynYYKgZYNkfW23bHH0bY9vKG:oIF7veINpKDFiaX70doFk\WyudXzhdkBld22jaX6gLG4yUUOGKTDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNUC9NE4xODB5NDFOwG0> MnXjNlQ6ODB4N{i=
CCRF-CEM cells M3n3d2Z2dmO2aX;uJIF{e2G7 NUm5OHZIOjRiaB?= MYHJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKEOFUl[tR2VOKGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEC3OkDPxE1? MnTzNlQ6ODB4N{i=
DLD1 cells MUfGeY5kfGmxbjDhd5NigQ>? NHTZb2MzPCCq MXfJcohq[mm2aX;uJI9nKGejbX3hMZNm[3KndHHz[UBu\WSrYYTl[EBkdGWjdnHn[UBw\iCQb4TjbEAyKGmwIHj1cYFvKESOREGgZ4VtdHNiYYPz[ZN{\WRiYYOgcpVkdGWjcjDhZ4N2dXWuYYTpc44hd2ZiTn;0Z4ghOSCrboTyZYNmdGy3bHHyJIRwdWGrbjCoUlFKS0RrIHHmeIVzKDJ2IHjyd{BjgSCHTFnTRUwhUUN3ME2wMlAxODl6IN88US=> MoOxNlQ6ODB4N{i=
A2780 cells NIX3bI5HfW6ldHnvckBie3OjeR?= NYjyeGl{OjRiaB?= NVTLc4t2UW6qaXLpeIlwdiCxZjDnZY1u[S2|ZXPy[ZRie2VibXXkbYF1\WRiY3zlZZZi\2Vib3[gUo91[2hiMTDpckBpfW2jbjDBNlc5OCClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTBwMECxNFMh|ryP M4jBd|I1QTByNke4
SUP-T1 cells MVTGeY5kfGmxbjDhd5NigQ>? Mnj5NlQhcA>? NEHDXFZKdmirYnn0bY9vKG:oIHfhcY1iNXOnY4LleIF{\SCvZXTpZZRm\CClbHXheoFo\SCxZjDOc5RkcCBzIHnuJIh2dWGwIGPVVE1VOSClZXzsd{Bie3Onc4Pl[EBieyCwdXPs[YFzKGGlY4XteYxifGmxbjDv[kBPd3SlaDCxJIlvfHKjY3XscJVt[XJiZH;tZYlvKCiQMVnDSEkh[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTBwMECxNlQh|ryP NVrkeoVlOjR7MEC2O|g>
Jurkat cells NI[0XmhHfW6ldHnvckBie3OjeR?= MX[yOEBp M2q5fmlvcGmkaYTpc44hd2ZiZ3HtcYEue2WlcnX0ZZNmKG2nZHnheIVlKGOuZXH2ZYdmKG:oIF7veINpKDFiaX6gbJVu[W5iSoXyb4F1KGOnbHzzJIF{e2W|c3XkJIF{KG63Y3zlZZIh[WOldX31cIF1cW:wIH;mJG5wfGOqIEGgbY51emGlZXzseYxieiCmb33hbY4hME5zSVPELUBi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yMEW5OUDPxE1? NG\sSWIzPDlyME[3PC=>

... 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