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EPZ015666(GSK3235025)
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。
EPZ015666(GSK3235025)图片
CAS NO:1616391-65-1
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)383.44
FormulaC20H25N5O3
CAS No.1616391-65-1;
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 60 mg/mL (156.5 mM)
Water: <1 mg/mL
Ethanol: 48 mg/mL (125.2 mM)
Solubility (In vivo)2% DMSO+30% PEG 300+ddH2O: 5 mg/mL
Synonyms

GSK-3235025; GSK 3235025; GSK3235025; EPZ-015666; EPZ 015666; EPZ015666.

Chemical Name: (S)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide

InChi Key: ZKXZLIFRWWKZRY-KRWDZBQOSA-N

InChi Code: InChI=1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-/m0/s1

SMILES Code: O=C(C1=NC=NC(NC2COC2)=C1)NC[C@H](O)CN3CC4=C(C=CC=C4)CC3

实验参考方法
In Vitro

In vitro activity: EPZ015666 (also known as GSK3235025, an analog of EPZ015866) is a potent, selective and orally bioavailable inhibitor of PRMT5 (protein arginine methyltransferase) enzymatic activity in biochemical assays with Ki of 5-22 nM, and shows>20,000-fold selectivity over other PMTs. EPZ015666 demonstrates broad selectivity against a panel of other histone methyltransferases. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models. EPZ015666 represents a validated chemical probe for further study of PRMT5 biology and arginine methylation in cancer and other diseases.


Kinase Assay: EPZ015666 (also known as GSK3235025, an analog of EPZ015866) is a potent, selective and orally bioavailable inhibitor of PRMT5 (protein arginine methyltransferase) enzymatic activity in biochemical assays with Ki of 5-22 nM, and shows>20,000-fold selectivity over other PMTs. EPZ015666 demonstrates broad selectivity against a panel of other histone methyltransferases.


Cell Assay: EPZ015666 shows potent cellular activity that blocks symmetric dimethylation of SmD3 and inhibit proliferation of MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) with IC50 of 96-904 nM. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range.

In VivoEPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models
Animal modelMCL (Z-138, and Maver-1) xenograft models
Formulation & DosageDissolved in 0.5 % MC; 200 mg/kg; p.o.
ReferencesNat Chem Biol. 2015 Jun;11(6):432-7.