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RO 4929097
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C22H20F5N3O3
- MW: 469.4
Description
Potent γ-secretase inhibitor (GSI; IC50 value 4 nM) targeting Notch signaling with in vivo efficacy in various tumor cells, showing >100-fold selectivity with respect to 75 other proteins of various types (receptors, ion channels, and enzymes). Treatment of HEK293 cells with RO4929097 caused a dose-dependent decrease in the amount of Aβ peptides secreted into the culture medium (EC50 value 14 nM), and a strong dose-dependent inhibition of Notch processing in a Notch cell-based reporter assay (EC50 value 5 nM).
More Information
| Parent CAS No. | 847925-91-1 |
|---|---|
| Chemical Name | (S)-2,2-dimethyl-N1-(6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N3-(2,2,3,3,3-pentafluoropropyl)malonamide |
| SMILES | C(N[C@@H]1C(=O)NC2=CC=CC=C2C2=CC=CC=C21)(=O)C(C)(C)C(NCC(F)(F)C(F)(F)F)=O |&1:2,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C22H20F5N3O3/c1-20(2,18(32)28-11-21(23,24)22(25,26)27)19(33)30-16-14-9-4-3-7-12(14)13-8-5-6-10-15(13)29-17(16)31/h3-10,16H,11H2,1-2H3,(H,28,32)(H,29,31)(H,30,33)/t16-/m0/s1 |
| InChiKey | OJPLJFIFUQPSJR-INIZCTEOSA-N |
| CID | 49867930 |
| Short Description | γ-Secretase inhibitor |
References
- C. Huynh et al. The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma. PLoS One. 2011;6(9):e25264.
- L. Luistro et al. Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties. Cancer Res. 2009 Oct 1;69(19):7672-80.
- M.M. Gounder et al. Moving forward one Notch at a time. J Clin Oncol. 2012 Jul 1;30(19):2291-3.
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