PF-9363

PF-9363 is an inhibitor of lysine acetyltransferase 6A (KAT6A), also known as monocytic leukemia zinc finger protein (MOZ) and KAT6B, also known as MOZ-related factor (MORF, Kis = 0.27 and 2.4 nM, respectively). It is selective for KAT6A and KAT6B over KAT7, KAT5, and KAT8 (Kis = 70, 420, and 670 nM, respectively). PF-9363 reduces the proliferation of, and the levels of acetylation of histone 3 lysine 23 (H3K23Ac) and lysine 14 (H3K14Ac) in, ZR-75-1 breast epithelial carcinoma cells (IC50s = 0.37, 0.85, and 120 nM, respectively). It reduces tumor levels of H3K23Ac and tumor volume without affecting body weight in a ZR-75-1 breast cancer mouse xenograft model when administered at doses of 0.03, 03, or 5 mg/kg per day. PF-9363 (1 mg/kg per day) reduces tumor volume and increases survival in a patient-derived xenograft (PDX) mouse model of breast cancer.Formal Name: 2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]-benzenesulfonamide. CAS Number: 2569009-58-9. Synonyms: CTx-648. Molecular Formula: C20H20N4O6S. Formula Weight: 444.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: O=S(NC1=NOC2=CC(CN3C=CC=N3)=CC(OC)=C21)(C4=C(OC)C=CC=C4OC)=O. InChi Code: InChI=1S/C20H20N4O6S/c1-27-14-6-4-7-15(28-2)19(14)31(25,26)23-20-18-16(29-3)10-13(11-17(18)30-22-20)12-24-9-5-8-21-24/h4-11H,12H2,1-3H3,(H,22,23). InChi Key: VNSQFPFWUAZOTQ-UHFFFAOYSA-N.