PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity.
IC50&Target
EZH2 WT
0.7 nM (Ki)
EZH2 Y641N
3.0 nM (Ki)
体外研究
PF-06726304 (Compound 31) inhibits H3K27me3 in Karpas-422 with an IC50 of 15 nM.
PF-06726304 inhibits the proliferation of Karpas-422 cells that harbor wild-type EZH2 with an IC50 of 25 nM.
体内研究
PF-06726304 (200 and 300 mg/kg; BID for 20 days) inhibits tumor growth and induces robust modulation of downstream biomarkers in a subcutaneous Karpas-422 xenograft model.
Animal Model:
Female Scid beige mice (6-8 weeks old) with Karpas-422 xenograft model
Dosage:
200 and 300 mg/kg
Administration:
Given BID for 20 days
Result:
Inhibited tumor growth and induced robust modulation of downstream biomarkers in a subcutaneous Karpas-422 xenograft model.
分子量
446.33
CAS号
1616287-82-1
运输条件
Room temperature in continental US; may vary elsewhere.