HJC0152 (hydrochloride)

HJC0152 is an orally bioavailable inhibitor of STAT3 (32 and 62% inhibition at 10 and 20 µM, respectively, in MDA-MB-231 cells in a luciferase reporter assay). It reduces total STAT3 and phosphorylated STAT3 levels in MDA-MB-231 cells and inhibits nuclear translocation of phosphorylated STAT3. HJC0152 inhibits proliferation of MCF-7 and MDA-MB-231 breast cancer and AsPC-1 and PANC-1 pancreatic cancer cells (IC50s = 0.91, 1.64, 1.9, and 1.08 µM, respectively). It also halts the cell cycle at the G0/G1 phase, induces apoptosis, and suppresses cell proliferation in human head and neck squamous cell carcinoma cells. HJC0152 (7.5 mg/kg, i.p. or 25 mg/kg, p.o.) inhibits tumor growth in an MDA-MB-231 breast cancer mouse xenograft model and in an orthotopic mouse model of squamous cell carcinoma.Formal Name: 2-(2-aminoethoxy)-5-chloro-N-(2-chloro-4-nitrophenyl)-benzamide, monohydrochloride. CAS Number: 1420290-99-8. Molecular Formula: C15H13Cl2N3O4 . HCl. Formula Weight: 406.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.1 mg/ml, DMSO: 2 mg/ml. lambdamax: 326 nm. SMILES: ClC1=C(NC(C2=C(OCCN)C=CC(Cl)=C2)=O)C=CC([N+]([O-])=O)=C1.Cl. InChi Code: InChI=1S/C15H13Cl2N3O4.ClH/c16-9-1-4-14(24-6-5-18)11(7-9)15(21)19-13-3-2-10(20(22)23)8-12(13)17,/h1-4,7-8H,5-6,18H2,(H,19,21),1H. InChi Key: XRZHLOYBZOONSZ-UHFFFAOYSA-N.