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Home > Inhibitors & Agonists > Epigenetics > Histone Methyltransferase (HMTase)

EPZ015666

  Cat. No.:  DC8012   Featured
Chemical Structure
1616391-65-1
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More than 5000 active chemicals with high quality for research!
Field of application
EPZ015666 is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1616391-65-1
Chemical Name: N-[(2S)-3-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide
Synonyms: EPZ015666;EPZ-015666;GSK3235025;GSK-3235025;(S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide;YQ36286;EPZ 015666;N-[(2s)-3-(3,4-Dihydroisoquinolin-2(1h)-Yl)-2-Hydroxypropyl]-6-(Oxetan-3-Ylamino)pyrimidine-4-Carboxamide;AK200926;3XV;GTPL8287;AOB5167;ZKXZLIFRWWKZRY-KRWDZBQOSA-N;BDBM177922;N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide;s7748;Z
SMILES: O1C([H])([H])C([H])(C1([H])[H])N([H])C1C([H])=C(C(N([H])C([H])([H])[C@@]([H])(C([H])([H])N2C([H])([H])C3=C([H])C([H])=C([H])C([H])=C3C([H])([H])C2([H])[H])O[H])=O)N=C([H])N=1
Formula: C20H25N5O3
M.Wt: 383.4442
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: EPZ015666 is an orally available inhibitor of PRMT5 with an IC50 of 22 nM.
In Vivo: EPZ015666 is orally bioavailable and amenable to in vivo studies. We performed 21-d efficacy studies in severe combined immunodeficiency (SCID) mice bearing subcutaneous Z-138 and Maver-1 xenografts, with twice-daily (BID) oral dosing on four dose groups: 25, 50, 100 and 200 mg per kilogram of body weight (mg/kg). After 21 d of continuous dosing, animals are euthanized, and blood and tissues are analyzed to determine the relationship between methyl-mark pharmacodynamics and tumor-growth inhibition (TGI). EPZ015666 showed dose-dependent exposure and TGI after 21 d in both MCL models. Tumors in all EPZ015666 dose groups measured on day 21 showed statistically significant differences in weight, volume and tumor growth compared to vehicle-treated tumors. Dosing at 200 mg/kg BID induced tumor stasis in Z-138 cells, with >93% TGI after 21 d, whereas Maver-1 cells showed >70% TGI. Additionally, a third MCL xenograft is tested using the Granta-519 cell line, a fast-growing model that reached endpoint on day 18 and showed dose-dependent efficacy with 45% TGI in the 200 mg/kg group. EPZ015666 is well tolerated in all three models, with minimal bodyweight loss in the 200 mg/kg dose group and no other clinical observations[1].
In Vitro: Treatment of MCL cell lines with EPZ015666 leads to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range[1]. EPZ015666, a potent peptide-competitive and SAM-cooperative inhibitor with >10,000-fold specificity against PRMT5 relative to other methyltransferases[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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