A-485

A-485 is an inhibitor of the histone acetyltransferase p300/CBP (IC50 = 60 nM). It decreases acetylated histone H3 lysine 27 (H3K27Ac), but not H3K9Ac, levels in PC3 cells in a concentration-dependent manner. A-485 reduces proliferation of non-small cell lung cancer (NSCLC), small cell lung cancer, triple-negative breast cancer, mantel cell lymphoma, multiple myeloma, non-Hodgkin's, and acute myeloid leukemia cell lines. It inhibits expression of prostate specific antigen (PSA) and H3K27Ac occupancy at the PSA enhancer without inhibiting androgen receptor occupancy in LNCaP-FGC cells. A-485 reduces tumor volume in a LuCaP-77 mouse xenograft model of castration-resistant prostate cancer when administered at a dose of 100 mg twice per day for 21 days.Formal Name: (1R)-N-[(4-fluorophenyl)methyl]-2,3-dihydro-5-[[(methylamino)carbonyl]amino]-2',4'-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]-spiro[1H-indene-1,5'-oxazolidine]-3'-acetamide. CAS Number: 1889279-16-6. Molecular Formula: C25H24F4N4O5. Formula Weight: 536.5. Purity: >98% (mixture of isomers). Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 16 mg/ml, Ethanol: 20 mg/ml, Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 253 nm. SMILES: O=C(NC)NC1=CC=C2C(CC[C@]23C(N(CC(N(CC4=CC=C(F)C=C4)[C@@H](C)C(F)(F)F)=O)C(O3)=O)=O)=C1. InChi Code: InChI=1S/C25H24F4N4O5/c1-14(25(27,28)29)32(12-15-3-5-17(26)6-4-15)20(34)13-33-21(35)24(38-23(33)37)10-9-16-11-18(7-8-19(16)24)31-22(36)30-2/h3-8,11,14H,9-10,12-13H2,1-2H3,(H2,30,31,36)/t14?,24-/m1/s1. InChi Key: VRVJKILQRBSEAG-PYFQUHSISA-N.