Cat. No.: HY-11102

RO4929097

20 Cited Publications

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Based on 20 publication(s) in Google Scholar

RO4929097 is an orally active γ secretase inhibitor with an IC₅₀ of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC₅₀ of 14 nM and 5 nM, respectively.

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Pureté: 98.64%
CAS No.: 847925-91-1
Formule: C₂₂H₂₀F₅N₃O₃
Masse moléculaire:469.40

Stockage:

4°C, stored under nitrogen

* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

RO4929097 Chemical Structure

CAS No.: 847925-91-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (20)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

RO4929097 is an orally active γ secretase inhibitor with an IC₅₀ of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC₅₀ of 14 nM and 5 nM, respectively^[1].

IC₅₀ & Target

IC50: 4 nM (γ secretase)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	14 nM Compound: 12; RO4929097	Inhibition of gamma secretase in HEK293 cells expressing APP695 assessed as reduction in amyloid beta (1 to 40 residues) by ELISA Inhibition of gamma secretase in HEK293 cells expressing APP695 assessed as reduction in amyloid beta (1 to 40 residues) by ELISA	[PMID: 27045975]
HEK293	EC₅₀	5 nM Compound: 12; RO4929097	Inhibition of gamma secretase mediated Notch1 signaling in HEK293 cells expressing truncated human Notch1 by luciferase reporter gene assay Inhibition of gamma secretase mediated Notch1 signaling in HEK293 cells expressing truncated human Notch1 by luciferase reporter gene assay	[PMID: 27045975]

In Vitro

RO4929097 inhibits the production of ICN reducing the expression of the downstream Notch target, Hes1, producing a less transformed morphology in A549 cells. RO4929097 inhibits Notch processing in human tumor-derived cells^[1].RO4929097 (1 μM) inhibits the growth of breast cancer cells, and the inhibition is 20% for SUM149 and 10% for SUM190 cells. RO4929097 does not have a marked effect in invasiveness of SUM149 cells. RO4929097 significantly reduces colony formation by both cell lines with the effect being more notable in SUM149 than by SUM190 cells^[2]. RO4929097 inhibits proliferation, anchorage independent growth, and sphere formation of primary melanoma cells in vitro^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RO4929097 (3-60 mg/kg, p.o.) results in significant tumor growth inhibition in nude mice bearing A549 NSCLC xenografts, compared with vehicle-treated animals. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially causes regression of established A549 tumors^[1]. RO4929097 impairs the growth of primary melanoma cells in vivo. The percentage of secondary tumors formed by RO4929097-treated cells is lower; the secondary tumors formed by RO4929097-treated cells are smaller; a significant delay in tumor formation by the RO4929097-treated cells compared to the vehicle-treated ones is observed in mice injected with 10⁴ cells in vivo^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 847925-91-1
Appearance Solid
Masse moléculaire 469.40
Formule C₂₂H₂₀F₅N₃O₃
Color White to off-white
SMILES

O=C(C(C)(C(NCC(F)(C(F)(F)F)F)=O)C)N[C@H]1C2=CC=CC=C2C3=CC=CC=C3NC1=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, stored under nitrogen

* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

Publications (20)

All Flow CytometryRT-PCRCell Migration/Invasion AssayWBCell Imaging/Staining

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Journal Impact Factor

Sci Bull

Tumor cell-derived N-acetyl-aspartyl-glutamate reshapes the tumor microenvironment to facilitate breast cancer metastasis. [Abstract]

2025 Apr 15;70(7):1126-1138. PMID: 39800628
Nat Commun

Chronic cerebral hypoperfusion induces venous dysfunction via EPAS1 regulation in mice. [Abstract]

2025 Jul 8;16(1):6302. PMID: 40628749
Theranostics

The hepatocyte-specifically expressed lnc-HSER alleviates hepatic fibrosis by inhibiting hepatocyte apoptosis and epithelial-mesenchymal transition. [Abstract]

2019 Oct 12;9(25):7566-7582. PMID: 31695787
J Exp Clin Cancer Res

Musashi2 contributes to the maintenance of CD44v6+ liver cancer stem cells via notch1 signaling pathway. [Abstract]

2019 Dec 30;38(1):505. PMID: 31888685
Cell Rep Med

CLDN4 palmitoylation promotes hepatic-to-biliary lineage transition and lenvatinib resistance in hepatocellular carcinoma. [Abstract]

2025 Jul 15;6(7):102208. PMID: 40592346
Cell Commun Signal

Presenilin1 inhibits glioblastoma cell invasiveness via promoting Sortilin cleavage. [Abstract]

2021 Nov 15;19(1):112. PMID: 34781973

RO4929097 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2021 Nov 15;19(1):112. [Abstract]

Transwell assays to detect the invasion ability of U87 and U251 cells when treated with RO4909497 alone, combined with AF38469 or with down-regulation of Sortilin in U87 and U251 cell.
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
J Transl Med

The stromal-tumor amplifying STC1-Notch1 feedforward signal promotes the stemness of hepatocellular carcinoma. [Abstract]

2023 Mar 31;21(1):236. PMID: 37004088
Cell Chem Biol

Discovery of a tau-aggregate clearing compound that covalently targets P4HB. [Abstract]

2025 Oct 16;32(10):1235-1248.e34. PMID: 41056949
Cell Chem Biol

Lenalidomide bypasses CD28 co-stimulation to reinstate PD-1 immunotherapy by activating Notch signaling. [Abstract]

2022 Aug 18;29(8):1260-1272.e8. PMID: 35732177
Neural Regen Res

Sox11b regulates the migration and fate determination of Müller glia-derived progenitors during retina regeneration in zebrafish. [Abstract]

2023 Feb;18(2):445-450. PMID: 35900444

RO4929097 purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2023 Feb;18(2):445-450. [Abstract]

qPCR showed the relative mRNA expression levels of sox11a and sox11b in PBS-or RO4929097(250 μM)-treated retinas at 4 dpi.

RO4929097 purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2023 Feb;18(2):445-450. [Abstract]

BrdU immunofluorescence showed that RO4929097 (250 μM)-treated MGPCs exhibited a more rounded morphology. Outlines of MGPC nuclei are indicated by white dotted lines.
Int J Mol Sci

Cdk4 Regulates Glioblastoma Cell Invasion and Stemness and Is Target of a Notch Inhibitor Plus Resveratrol Combined Treatment. [Abstract]

2023 Jun 13;24(12):10094. PMID: 37373242

RO4929097 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Jun 13;24(12):10094. [Abstract]

Flow cytometry analysis of U87MG-N CD44+ and T98G-N CD133+ subpopulations cultured in the presence of vehicle (-) or RSV+ (GSI) (2 μM).

RO4929097 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Jun 13;24(12):10094. [Abstract]

U87MG and T98G cells were treated with vehicle (-) or 10 μM RSV and/or 2 μM RO4929097 (GSI) for 24 h, and immunoblotting was carried out.
FASEB J

MiR-2392 suppresses metastasis and epithelial-mesenchymal transition by targeting MAML3 and WHSC1 in gastric cancer. [Abstract]

2017 Sep;31(9):3774-3786. PMID: 28512191

RO4929097 purchased from MedChemExpress. Usage Cited in: FASEB J. 2017 Sep;31(9):3774-3786. [Abstract]

Western blot analysis of E-cadherin, vimentin, Slug, and Twist1 in BGC823 cells treated with RO4929097 in addition to miR-2392 inhibition.
ACS Med Chem Lett

High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma. [Abstract]

2015 Jun 22;6(8):948-52. PMID: 26288699
Sci Rep

The neuroepithelial origin of ovarian carcinomas explained through an epithelial-mesenchymal-ectodermal transition enhanced by cisplatin. [Abstract]

2024 Nov 26;14(1):29286. PMID: 39592661
J Biol Chem

Individual and combined presenilin 1 and 2 knockouts reveal that both have highly overlapping functions in HEK293T cells. [Abstract]

2019 Jul 19;294(29):11276-11285. PMID: 31167792
Development

Alveolar progenitor differentiation and lactation depends on paracrine inhibition of notch via ROBO1/CTNNB1/JAG1. [Abstract]

2021 Nov 1;148(21):dev199940. PMID: 34758082
Oncol Lett

Notch3 is involved in the proliferation of renal cancer cells via regulation of cell cycle progression and HIF-2α. [Abstract]

2020 Dec;20(6):379. PMID: 33154777
bioRxiv

Human ectodermal organoids reveal the cellular origin of DiGeorge Syndrome. [Abstract]

2025 Aug 8:2025.08.08.669417. PMID: 40855884
Patent

US20180263995A1.

Solvant et solubilité

In Vitro:

DMSO : ≥ 49 mg/mL (104.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1304 mL

10.6519 mL

21.3038 mL

5 mM

0.4261 mL

2.1304 mL

4.2608 mL

10 mM

0.2130 mL

1.0652 mL

2.1304 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[2]

The IBC cell lines SUM149 and SUM190 are seeded at a density of 5 × 10⁴ cells. The next day, they are treated with vehicle or increasing doses of RO4929097, ranging from 0.1 nM to 10 μM. After 72 hrs, cells are trypsinized and viable cells counted with a hemocytometer.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice: RO4929097-treated mice are orally dosed with suspensions at 3 to 60 mg/kg RO4929097 according to the indicated regimens. In the Calu-6 xenograft model, RO4929097 is dosed at 60 mg/kg/d every other week for 4 weeks (7+/7- × 2 cycles). For all other xenograft models, RO4929097 is dosed once daily at 10 mg/kg for 21 days. Statistical analysis is determined by Mann-Whitney rank-sum test, one-way ANOVA, and post hoc Bonferroni t test. Differences between groups are considered significant when P ≤ 0.05. A549 tumors from vehicle-treated and selected RO4929097-treated groups are collected and fixed in 10% zinc-formalin overnight, processed, paraffin-embedded, sectioned at 5 μM, and stained with H&E for histopathology assessment. An Olympus BX51 microscope (×40 objective) mounted with a Nikon DS-Fi1 using the NIS-Elements F2.20 program collected the histology pictures. For Western blot analysis, three A549 tumors from each group, 7 (60 mg/kg) or 21 days (3 and 30 mg/kg), are flash-frozen. Collagen type V is detected using the H-200 antibody at a dilution of 1:1,000, and MFAP5 is detected using the antibody at a dilution of 1:1,000.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (284 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Luistro L, et al. Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties. Cancer Res. 2009, 69(19), 7672-7680. [Content Brief]

[2]. Debeb BG, et al. Pre-clinical studies of Notch signaling inhibitor RO4929097 in inflammatory breast cancer cells. Breast Cancer Res Treat. 2012. [Content Brief]

[3]. Huynh C, et al. The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma. PLoS One. 2011, 6(9), e25264. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1304 mL	10.6519 mL	21.3038 mL	53.2595 mL
	5 mM	0.4261 mL	2.1304 mL	4.2608 mL	10.6519 mL
	10 mM	0.2130 mL	1.0652 mL	2.1304 mL	5.3259 mL
	15 mM	0.1420 mL	0.7101 mL	1.4203 mL	3.5506 mL
	20 mM	0.1065 mL	0.5326 mL	1.0652 mL	2.6630 mL
	25 mM	0.0852 mL	0.4261 mL	0.8522 mL	2.1304 mL
	30 mM	0.0710 mL	0.3551 mL	0.7101 mL	1.7753 mL
	40 mM	0.0533 mL	0.2663 mL	0.5326 mL	1.3315 mL
	50 mM	0.0426 mL	0.2130 mL	0.4261 mL	1.0652 mL
	60 mM	0.0355 mL	0.1775 mL	0.3551 mL	0.8877 mL
	80 mM	0.0266 mL	0.1331 mL	0.2663 mL	0.6657 mL
	100 mM	0.0213 mL	0.1065 mL	0.2130 mL	0.5326 mL

Keywords

RO4929097

20 Cited Publications

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RO4929097

Neuronal Signaling Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Neurodegenerative Disease-related Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Publications Citing Use of MedChemExpress (MCE) RO4929097

Activité biologique

Chemical Information

Publications (20)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

RO4929097 Related Classifications

HY-11102 Related Classifications