GSK3368715 (hydrochloride)

GSK3368715 is an inhibitor of type I protein arginine methyltransferases (PRMTs, IC50s = 3.1, 162, 38, 4.7, and 39 nM for PRMT1, 3, 4, 6, and 8, respectively). It is selective for type I PRMTs over PRMT5, 7, and 9 (IC50s = >20,408, >40,000, and >15,000 nM, respectively), as well as 20 additional methyltransferases and a panel of ion channels, receptors, and transporters at 10 µM. GSK3368715 (5 µM) inhibits the growth of patient-derived diffuse large B cell lymphoma (DLBCL) cells. In vivo, GSK3368715 (9.375-150 mg/kg) reduces tumor volume in Toledo DLBCL and BxPC-3 pancreatic adenosarcoma mouse xenograft models. It also reduces tumor growth in ACHN renal carcinoma and MDA-MB-468 breast cancer mouse xenograft models and a pancreatic adenocarcinoma patient-derived xenograft (PDX) mouse model when administered at doses of 150 and 300 mg/kg, respectively.Formal Name: N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-1,2-ethanediamine, monohydrochloride. CAS Number: 2227587-25-7. Molecular Formula: C20H38N4O2 . HCl. Formula Weight: 403.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 40 mg/ml. SMILES: CN(CCNC)CC1=CNN=C1C2CCC(COCC)(COCC)CC2.Cl. InChi Code: InChI=1S/C20H38N4O2.ClH/c1-5-25-15-20(16-26-6-2)9-7-17(8-10-20)19-18(13-22-23-19)14-24(4)12-11-21-3,/h13,17,21H,5-12,14-16H2,1-4H3,(H,22,23),1H. InChi Key: WRVJUOWIQSTJPE-UHFFFAOYSA-N.