RO 4929097 New
Tocris Bioscience, part of Bio-Techne | Catalog # 8906
Potent and selective γ-secretase inhibitor; also induces differentiation of iEM cells into luminal cells
Key Product Details
Description
Potent and selective γ-secretase inhibitor; also induces differentiation of iEM cells into luminal cells
Alternative Names
RG-4733
Product Description
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.Product Specifications
Molecular Weight
469.41
Formula
C22H20F5N3O3
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 | 21.30 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Loh Protocol for efficient generation of human artery and vein endothelial cells from pluripotent stem cells STAR Protoc. 2025 PMID: 39705146
- Sahebjam A phase I study of the combination of ro4929097 and cediranib in patients with advanced solid tumours (PJC-004/NCI 8503). BJC 2013 PMID: 23868004
- Huynh The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma. PLOS One 2011 PMID: 21980408
- Hayakawa Establishment and characterization of immortalized sweat gland myoepithelial cells. Sci.Rep 2022 PMID: 34997030
- Luistro Preclinical profile of a potent γ-Secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties. Cancer Res. 2009 PMID: 19773430
Product Specific Notices for RO 4929097
For research use only
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