SML1421

EPZ015666

≥98% (HPLC)

• Synonyme(s) : (S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide, GSK3235025, YQ36286
• Formule empirique (notation de Hill) : C₂₀H₂₅N₅O₃
• CAS Number: 1616391-65-1
• Poids moléculaire : 383.44
• Numéro MDL: MFCD28411588
• Code UNSPSC : 12352200
• ID de substance PubChem : 329825864
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 20 mg/mL, clear
• Température de stockage: 2-8°C
• Chaîne SMILES: O[C@H](CN1CCC(C=CC=C2)=C2C1)CNC(C3=CC(NC4COC4)=NC=N3)=O
• 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
• Clé InChI: ZKXZLIFRWWKZRY-KRWDZBQOSA-N

Description

Actions biochimiques/physiologiques

EPZ015666 (GSK3235025) is a protein arginine methyltransferase PRMT5 inhibitor with an IC₅₀ value of of 22 nM in biochemical assays and no inhibition up to the maximum tested concentration of 50 μM against a panel of 20 other protein methyltransferases. Inhibition was uncompetitive with respect to SAM. EPZ015666 showed dose-dependent antitumor activity in multiple in vitro and in vivo mantle cell lymphoma (MCL) models with treatment of MCL cell lines leading to inhibition of SmD3 methylation and cell death.

EPZ015666 (GSK3235025) is a protein arginine methyltransferase PRMT5 inhibitor.

Autres remarques

EPZ015666 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the EPZ015666 probe summary on the Chemical Probes Portal website.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable