| CAS NO: | 1616392-22-3 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 452.55 |
|---|---|
| Formula | C24H32N6O3 |
| CAS No. | 1616392-22-3 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 90 mg/mL (198.8 mM) |
| Water:<1 mg/mL | |
| Ethanol: 90 mg/mL (198.8 mM) | |
| Solubility (In vivo) | 2.2 mg/mL in 10% DMSO : 40% PEG300 : 5% Tween-80 : 45% saline |
| Synonyms | EPZ-015938; EPZ 015938; EPZ015938; Pemrametostat; GSK3326595; GSK 3326595; GSK-3326595; Chemical Name: (S)-6-((1-acetylpiperidin-4-yl)amino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)pyrimidine-4-carboxamide |
| SMILES Code | O=C(C)N1CCC(NC2=NC=NC(C(NC[C@H](O)CN3CCC(C=CC=C4)=C4C3)=O)=C2)CC1 |
| In Vitro | In vitro activity: GSK3326595 (formerly known as EPZ015938) is an orally bioactive, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It potently inhibits tumor growth in vitro and in vivo in animal models. GSK3326595 is able to halt cell proliferation and induce apoptosis in numerous solid and hematologic tumor cell lines. It has demonstrated potent in vivo anti-tumor activity in animal models. The protein arginine methyltransferases (PRMT) are a family of 11 enzymes that catalyze mono- or dimethylation of arginine residues on histones. so far PRMT inhibitors (PRMTi) are still limited to preclinical studies. Kinase Assay: GSK3326595 (formerly known as EPZ015938) is an orally bioactive, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). Cell Assay: GSK3326595 is able to halt cell proliferation and induce apoptosis in numerous solid and hematologic tumor cell lines. I |
|---|---|
| In Vivo | GSK3326595 has demonstrated potent in vivo anti-tumor activity in animal models. The protein arginine methyltransferases (PRMT) are a family of 11 enzymes that catalyze mono- or dimethylation of arginine residues on histones. so far PRMT inhibitors (PRMTi) are still limited to preclinical studies. |
| Animal model | |
| Formulation & Dosage | |
| References | Biomolecules. 2017 Mar; 7(1): 3; WO 2016022605 A1 |
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