AZD 9496

AZD 9496 is a potent and selective estrogen receptor downregulator (SERD) with an IC50 value of 0.138 nM for estrogen receptor alpha (ERalpha) downregulation. It is selective for ERalpha compared to other nuclear hormone receptors with IC50 values of 0.0008, 0.54, 9.2, and 30 µM for ERalpha, progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR), respectively. AZD 9496 decreases ERalpha activity (IC50 = 0.282 nM), measured via quantification of downstream PR activity, and reduces proliferation of MCF-7 breast cancer cells (IC50 = 0.0398 nM). It also inhibits MCF-7 xenograft growth in mice in a dose-dependent manner.Formal Name: (2E)-3-[3,5-difluoro-4-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-1H-pyrido[3,4-b]indol-1-yl]phenyl]-2-propenoic acid. CAS Number: 1639042-08-2. Molecular Formula: C25H25F3N2O2. Formula Weight: 442.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:6): 0.14 mg/mL. lambdamax: 225, 276 nm. SMILES: CC(F)(C)CN1[C@H](C)CC2=C(NC3=C2C=CC=C3)[C@H]1C4=C(F)C=C(/C=C/C(O)=O)C=C4F. InChi Code: InChI=1S/C25H25F3N2O2/c1-14-10-17-16-6-4-5-7-20(16)29-23(17)24(30(14)13-25(2,3)28)22-18(26)11-15(12-19(22)27)8-9-21(31)32/h4-9,11-12,14,24,29H,10,13H2,1-3H3,(H,31,32)/b9-8+/t14-,24-/m1/s1. InChi Key: DFBDRVGWBHBJNR-BBNFHIFMSA-N.