Catalog No.S1575

RO4929097 Chemical Structure

Molecular Weight(MW): 469.4

RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.

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In DMSO USD 238 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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Cited by 26 Publications

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Biological Activity

Description RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.
γ secretase [1]
(Cell-free assay)
γ secretase(ICN) [1]
(Cell-free assay)
Aβ40 [1]
(Cell-free assay)
4 nM 5 nM 14 nM
In vitro

RO4929097 decreases the amount of Aβ peptides secreted into the culture medium in HEK293 cells with EC50 of 14 nM. RO4929097 strongly inhibits Notch processing with EC50 of 5 nM in the Notch cell-based reporter assay. The potency of RO4929097 in cell-free and cellular assays is in the low nanomolar range with >100-fold selectivity observed with respect to 75 other proteins of various types including receptors, ion channels, and enzymes (CEREP panel). After 5 days of treatment, RO4929097 reduces the production of ICN in the human NSCLC A549 cells inducing a flattened and less transformed tumor cell phenotype in tissue culture. [1] RO4929097 blocks Notch processing in human non-small cell lung carcinoma cells and decreases expression of the Notch transcriptional target gene Hes1. Treatment with RO4929097 reveals a two- to threefold decrease in the expression of direct Notch target genes, Hes1, Hey1, and Heyl in SUM149 and a 3.5- to eightfold decrease in expression in SUM190 cells. RO4929097 modestly inhibits the growth of SUM149 cells in a dose-dependent manner. At a concentration of 1 μM of RO4929097, growth inhibition is 20 % for SUM149 and 10 % for SUM190 cells, relative to vehicle-treated controls. RO4929097 decreases the production of inflammatory cytokines by T-cells. Furthermore, with RO4929097 treatment, there is a shift in favor of TH2 over TH1 cytokines. In addition, T-cell activation induced IL-6 production would be increased with RO4929097. [2] Upon RO4929097 treatment, the selected melanoma cell lines reveals downregulation of NOTCH downstream effector HES1. A decrease in the amount of melanospheres formed upon RO4929097 treatment in primary melanoma cell lines is detected. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87 MlzaR4VtdCCYaXHibYxqfHliQYPzZZk> Ml3KN|Ah|ryP MUe0JIQ> NUDqTVln\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5 MVeyOFQ6PTlyNx?=
U87 R1 NXXFcW5US2WubDDWbYFjcWyrdImgRZN{[Xl? NV:1T4hUOzBizszN M3y3blQh\A>? NULkSmNm\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5 MVOyOFQ6PTlyNx?=
MGG4 MlnyR4VtdCCYaXHibYxqfHliQYPzZZk> M1noSlMxKM7:TR?= NX22cYgyPCCm NH7m[FNl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= M{CyVFI1PDl3OUC3
MGG6 M1qzfGNmdGxiVnnhZoltcXS7IFHzd4F6 MmDwN|Ah|ryP MlniOEBl NGDYeZJl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= MmDZNlQ1QTV7MEe=
MGG8 NFuyO2xE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXLqeFVbOzBizszN NFLFWIU1KGR? MX;k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? MnixNlQ1QTV7MEe=
MGG23 NFPxXHFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2nxdFMxKM7:TR?= MV60JIQ> NFjob4Zl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= NFPjWnAzPDR7NUmwOy=>
SUM149 MnzhR4VtdCCYaXHibYxqfHliQYPzZZk> NHvPTZMxNTFyIN88US=> NWfiRmljPzJiaB?= NETj[m5qdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 Moi2NlI2PDdzMEm=
Sum190 MUTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWDlUZRQOC1zMDFOwG0> M2K2OFczKGh? MlqxbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M4XsZlIzPTR5MUC5
WM98.1 NH7mOmtHfW6ldHnvckBCe3OjeR?= M3jHfVExKHWP NUnI[5kxOjRiaB?= MUTEUXNQ M1\JO4Rm[3KnYYPld{B1cGVibHX2[Yx{KG:oIF7PWGNJKGSxd37zeJJm[W1idHHy[4V1KEiHU{G= MV[yNVk5ODRyOB?=
WM115 NF7KPWVHfW6ldHnvckBCe3OjeR?= M2nnS|ExKHWP Mnf1NlQhcA>? MULEUXNQ NV7ufZFN\GWlcnXhd4V{KHSqZTDs[ZZmdHNib3[gUm9VS0hiZH;3cpN1emWjbTD0ZZJo\XRiSFXTNS=> MkXGNlE6QDB2MEi=
WM983A Ml;DSpVv[3Srb36gRZN{[Xl? NEK0fpQyOCC3TR?= NVvJVldiOjRiaB?= Mn7HSG1UVw>? M17pO4Rm[3KnYYPld{B1cGVibHX2[Yx{KG:oIF7PWGNJKGSxd37zeJJm[W1idHHy[4V1KEiHU{G= MnftNlE6QDB2MEi=
WM3248  M4nIWGZ2dmO2aX;uJGF{e2G7 M3;SXVExKHWP Mm\uNlQhcA>? NYTVXFNGTE2VTx?= Ml\E[IVkemWjc3XzJJRp\SCuZY\lcJMhd2ZiTl;UR2gh\G:5boP0doVidSC2YYLn[ZQhUEWVMR?= Mn\KNlE6QDB2MEi=
WM35 M4izPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jYelExKHWP MYmwMVE5KGR? NX:xWlJTTE2VTx?= MVrpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MnzLNlE6QDB2MEi=
WM98.1 NVS3VHdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVixNEB2VQ>? MkixNE0yQCCm Mom2SG1UVw>? MYXpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NFPWUmYzOTl6MESwPC=>
WM115 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLv[mZqOTBidV2= MYmwMVE5KGR? NFy1XZVFVVOR NELN[3hqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MVSyNVk5ODRyOB?=
WM983A M4jRTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1eyZlExKHWP NWH0eWZEOC1zODDk MVfEUXNQ MWjpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MXuyNVk5ODRyOB?=
WM3248  M32xUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnuyNVAhfU1? MViwMVE5KGR? MWXEUXNQ MXTpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 Ml7sNlE6QDB2MEi=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot

PubMed: 29899322     

HeLa and Caski cells treated with RO4929097 and the DMSO control showed downregulation of the Hey1 protein as determined by Western blot analysis;

Snail / N-cadherin / Twist / E-cadherin; 

PubMed: 29899322     

Effect of inhibiting the Notch signaling pathway on the protein expression levels of EMT-associated proteins Snail, N-cadherin, Twist, and E-cadherin in HeLa and Caski cells. 

Akt / p-Akt / Notch / IGF1R / FBXW7 ; 

PubMed: 28507201     

Western blots showing expression of p-Akt, Akt, Notch, IGF1R, and FBXW7 in HCC827/ER cells treated with MK-2206 (an Akt inhibitor) or RO4929097 (a Notch inhibitor). GAPDH served as an internal control. 

NICD / Hes1 / Hes3 / Hes5; 

PubMed: 24038660     

A panel of GICs was treated with the indicated doses of DAPT, BMS-708163 and RO4929097 for 48 hours. γ Secretase inhibitors inhibited expression of NICD, Hes1, Hes3 and Hes5 in a dose-dependent manner.

29899322 28507201 24038660
Growth inhibition assay
Cell viability; 

PubMed: 30669546     

A panel of GIC lines was treated with various concentrations of the RO4929097. Cells were treated in triplicate wells for 72 h, and cell viability was assessed with the CellTiter-Blue assay. Cell viability in the vehicle control was considered to be 100%; 

In vivo Oral injection of 3 to 60 mg/kg RO4929097 once daily or twice daily to nude mice bearing A549 NSCLC xenografts for either 7, 14, or 21 days of a 21-day schedule results in significant tumor growth inhibition compared with vehicle-treated animals. The tumor growth inhibition values ranges from 66% to 91%. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially arouses regression of established A549 tumors. At the end of the 21-day cycle (day 47), tumor growth prevention is still 91% compared with vehicle control mice. Inhibition of tumor growth remains prolonged and sustained up to 34 days post-treatment (day 67). On day 67, these mice are retreated with the same dose of RO4929097 for a second cycle (7 days) until day 74. Importantly, the antitumor effects are sustained after dosing is completed. [1] RO4929097 leads to reduced expression of genes associated with angiogenesis in A549 xenograft model. In contrast, the RO4929097-resistant H460a xenograft displays little change in expression of these genes, underscoring the in vivo anti-angiogenesis mechanism of action of RO4929097.[2] For IL6 and IL8 overexpressing tumors, RO4929097 no longer impacts angiogenesis or the infiltration of tumor associated fibroblasts. [4]


Kinase Assay:[5]
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In vitro potency assays:

After RO4929097 is used, the Aβ peptides are measured by ECL assays using a variety of anti-Aβ antibodies and an Origen 1.5 Analyzer. The 4G8 murine mAb binds an epitope in the Aβ peptide (within amino acids 18–21) that is immediately distal to the α-secretase cleavage site. The G2–10 murine mAb binds the C terminus that is exposed after γ-secretase-mediated cleavage to generate amino acid 40 of the Aβ40 peptide. The FCA3542 rabbit antibody binds the C terminus that is exposed after γ-secretase-mediated cleavage to generate amino acid 42 of the Aβ42 peptide. The 4G8 mAb is biotinylated with biotin-LC-sulfo-N-hydroxysuccinimide-ester. The G2–10 and FCA3542 antibodies are ruthenylated with TAG-N-hydroxysuccinimide ester. Aβ(x-40) is detected with biotinylated 4G8 and ruthenylated G2–10. Aβ(x-42) is detected with biotinylated 4G8 and ruthenylated FCA3542.
Cell Research:[3]
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  • Cell lines: WM35 and WM98.1 cell lines
  • Concentrations: 10 μM
  • Incubation Time: DMSO
  • Method: Primary melanoma cell lines, including WM35 and WM98.1, are seeded at 2.5 × 103 cells per well on a 12-well dish in triplicate. The day after (day 0), the medium is replaced, and DMSO or 10 μM RO4929097 is added and changed every 3-4 days. At the indicated time points, cells are fixed in 10% formalin solution and stored in PBS at 4 °C. At day 18-24, all the plates are stained with crystal violet. After color elution with 10% acetic acid, optical density is read at 590 nm.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female nude mice bearing Calu-6 cells
  • Formulation: 1.0% Klucel in water with 0.2% Tween 80
  • Dosages: 3 to 60 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 93 mg/mL (198.12 mM)
Ethanol 16 mg/mL (34.08 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween+ddH2O
For best results, use promptly after mixing.

* 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 469.4


CAS No. 847925-91-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01269411 Terminated Adult Anaplastic Oligodendroglioma|Adult Brain Stem Glioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Recurrent Adult Brain Tumor National Cancer Institute (NCI) July 2011 Phase 1
NCT01269411 Terminated Adult Anaplastic Oligodendroglioma|Adult Brain Stem Glioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Recurrent Adult Brain Tumor National Cancer Institute (NCI) July 2011 Phase 1
NCT01238133 Terminated Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) December 2010 Phase 1
NCT01122901 Terminated Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor National Cancer Institute (NCI) December 2010 Phase 2
NCT01251172 Withdrawn DS Stage I Plasma Cell Myeloma|DS Stage II Plasma Cell Myeloma|DS Stage III Plasma Cell Myeloma|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) December 2010 Phase 2
NCT01270438 Withdrawn Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum|Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer National Cancer Institute (NCI) December 2010 Phase 2

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Frequently Asked Questions

  • Question 1:

    How about the half-life of RO4929097(S1575)?

  • Answer:

    For S1575, the half-life is about 20 hours based on the following paper:

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID