Ro 4929097

Ro 4929097 is a potent inhibitor of gamma-secretase (IC50 = 4 nM) that blocks both Abeta40 and Notch processing (IC50s = 14 and 5 nM, respectively). It displays greater than 100-fold selectivity for gamma-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype. It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation. Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.Formal Name: N1-[(7S)-6,7-dihydro-6-oxo-5H-dibenz[b,d]azepin-7-yl]-2,2-dimethyl-N3-(2,2,3,3,3-pentafluoropropyl)-propanediamide. CAS Number: 847925-91-1. Molecular Formula: C22H20F5N3O3. Formula Weight: 469.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.1 mg/ml, DMSO: 15 mg/ml, Ethanol: 10 mg/ml. lambdamax: 230 nm. SMILES: O=C(C(C)(C)C(NCC(F)(F)C(F)(F)F)=O)N[C@@H]1C(NC2=C(C=CC=C2)C3=C1C=CC=C3)=O. InChi Code: 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. InChi Key: OJPLJFIFUQPSJR-INIZCTEOSA-N.