CAS NO: | 2227587-25-7 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
Cas No. | 2227587-25-7 |
Canonical SMILES | CN(CCNC)CC1=CNN=C1C2CCC(COCC)(COCC)CC2.Cl |
分子式 | C20H38N4O2·HCl |
分子量 | 403 |
溶解度 | DMSO: 40 mg/ml |
储存条件 | -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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).1It 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. 1.Fedoriw, A., Rajapurkar, S.R., O’Brien, S., et al.Anti-tumor activity of the type I PRMT inhibitor, GSK3368715, synergizes with PRMT5 inhibition through MTAP lossCancer Cell36(1)100-114.e125(2019) |