Crenigacestat

Crenigacestat is an orally bioavailable Notch inhibitor. It induces cell cycle arrest at the G0/G1 phase and decreases expression of the oncogenes MYC and CCNA1 in Caki human renal cancer cells. Crenigacestat (8 mg/kg per day) reduces tumor growth and increases survival in a 769-P mouse xenograft model.Formal Name: N-[(1S)-2-[[(7S)-6,7-dihydro-5-(2-hydroxyethyl)-6-oxo-5H-pyrido[3,2-a][3]benzazepin-7-yl]amino]-1-methyl-2-oxoethyl]-4,4,4-trifluoro-butanamide. CAS Number: 1421438-81-4. Synonyms: LY3039478. Molecular Formula: C22H23F3N4O4. Formula Weight: 464.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 10 mg/ml, PBS (pH 7.2): 0.5 mg/ml. lambdamax: 227 nm. SMILES: O=C1[C@@H](NC([C@H](C)NC(CCC(F)(F)F)=O)=O)C2=CC=CC=C2C3=C(N=CC=C3)N1CCO. InChi Code: InChI=1S/C22H23F3N4O4/c1-13(27-17(31)8-9-22(23,24)25)20(32)28-18-15-6-3-2-5-14(15)16-7-4-10-26-19(16)29(11-12-30)21(18)33/h2-7,10,13,18,30H,8-9,11-12H2,1H3,(H,27,31)(H,28,32)/t13-,18-/m0/s1. InChi Key: YCBAQKQAINQRFW-UGSOOPFHSA-N.