Biological Activity
RO4929097 is an orally-bioavailable, potent and selective inhibitor of γ-secretase (IC50= 4 nM), producing inhibitory activity of Notch signaling in tumor cells. The potency of RO4929097 in cell-free and cellular assays is in low nanomolar range with >100-fold selectivity with respect to 75 other proteins of various types including receptors, ion channels, and enzymes. RO4929097 does not block tumor cell proliferation or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype. It is currently undergoing phase I dose escalation in patients with solid tumors [1-2].
Chemical Properties
| Cas No.: 847925-91-1 | M. Wt.: 469.40 |
| Formula: C22H20F5N3O3 | Purity: ≥98% |
| Synonym: RO-4929097, R4733 | |
| 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-pentafluoro-propyl)-malonamide | |
| Appearance: White solid | |
| Solubility: Souble in DMSO up to 50 mM | |
| Storage: Store solid at 4 ºC desiccated. Following reconstitution, aliquot and freeze at -20 ºC, prevent from multiple freeze/thaw cycles | |
