EPZ015666 (GSK3235025) 是有口服活性的 PRMT5抑制剂，IC₅₀ 为 22 nM。

EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 with an IC 50 of 22 nM.

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IC50: 22 nM (PRMT5)

Treatment of MCL cell lines with EPZ015666 (GSK3235025) leads to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. EPZ015666 (GSK3235025), a potent peptide-competitive and SAM-cooperative inhibitor with >10,000-fold specificity against PRMT5 relative to other methyltransferases. has not independently confirmed the accuracy of these methods. They are for reference only.

EPZ015666 (GSK3235025) 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 (GSK3235025) showed dose-dependent exposure and TGI after 21 d in both MCL models. Tumors in all EPZ015666 (GSK3235025) 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,

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Chan-Penebre E, et al. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nat Chem Biol. 2015 Jun;11(6):432-7.
[2]. Kryukov GV, et al. MTAP deletion confers enhanced dependency on the PRMT5 arginine methyltransferase in cancer cells. Science. 2016 Mar 11;351(6278):1214-8.

In Vitro: DMSO : 100 mg/mL (260.80 mM; Need ultrasonic)配制储备液