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Description: Potent and selective γ-secretase inhibitor; also induces differentiation of iEM cells into luminal cells
Alternative Names: RG-4733
Chemical Name: 2,2-Dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N'-(2,2,3,3,3-pentafluoropropyl)malonamide
Purity: ≥98% (HPLC)
Biological Activity for RO 4929097
RO 4929097 is a potent and selective γ-secretase inhibitor (IC50 = 4 nM), exhibiting over 100-fold selectivity against a panel of 75 different proteins. Inhibits cellular processing of Notch and Aβ40 (IC50 = 5 nM and 14 nM, respectively). In tumor cells, inhibition of Notch processing results in lowered expression of HES1. In multiple xenograft models, RO 4929097 displays antitumour effects with no associated body weight loss or Notch-related toxicities. In melanoma cell lines, it inhibits tumor formation and blocks invasive growth pattern of metastatic melanoma. Can also be used to induce differentiation of iEM cells into luminal cells. Orally bioavailable.
Technical Data for RO 4929097
| M. Wt | 469.41 |
| Formula | C22H20F5N3O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 847925-91-1 |
| PubChem ID | 49867930 |
| InChI Key | OJPLJFIFUQPSJR-INIZCTEOSA-N |
| Smiles | O=C(N[C@H]1C2=CC=CC=C2C3=CC=CC=C3NC1=O)C(C)(C)C(NCC(F)(F)C(F)(F)F)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for RO 4929097
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.47 | 50 | |
| ethanol | 23.47 | 50 |
Preparing Stock Solutions for RO 4929097
The following data is based on the product molecular weight 469.41. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.26 mL | 21.3 mL | 42.61 mL |
| 2.5 mM | 0.85 mL | 4.26 mL | 8.52 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.26 mL |
| 25 mM | 0.09 mL | 0.43 mL | 0.85 mL |
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Product Datasheets for RO 4929097
References for RO 4929097
References are publications that support the biological activity of the product.
Luistro et al (2009) Preclinical profile of a potent γ-Secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties. Cancer Res. 69 7672 PMID: 19773430
Huynh et al (2011) The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma. PLOS One 6 PMID: 21980408
Hayakawa et al (2022) Establishment and characterization of immortalized sweat gland myoepithelial cells. Sci.Rep 12 PMID: 34997030
Sahebjam et al (2013) A phase I study of the combination of ro4929097 and cediranib in patients with advanced solid tumours (PJC-004/NCI 8503). BJC 109 943 PMID: 23868004
Loh et al (2025) Protocol for efficient generation of human artery and vein endothelial cells from pluripotent stem cells STAR Protoc. 6 PMID: 39705146
If you know of a relevant reference for RO 4929097, please let us know.
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