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GSK3368715(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK3368715(hydrochloride)图片
CAS NO:2227587-25-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
An inhibitor of type I PRMTs
Cas No.2227587-25-7
Canonical SMILESCN(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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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)