PF-06726304 是选择性EZH2有效抑制剂，具有强抗肿瘤生长活性。它抑制野生型和 Y641N 突变型 EZH2，Ki分别为 0.7 和 3.0 nM。
产品描述
PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 (Kis: 0.7 and 3.0 nM, respectively).
体外活性
PF-06726304 suppresses the proliferation of Karpas-422 cells that harbor wild-type EZH2 (IC50: 25 nM). PF-06726304 suppresses H3K27me3 in Karpas-422 (IC50: 15 nM) [1].
体内活性
In a subcutaneous Karpas-422 xenograft model, PF-06726304 (200 and 300 mg/kg; BID for 20 days) suppresses tumor growth and causes robust modulation of downstream biomarkers[1].
Cas No.
1616287-82-1
分子式
C22H21Cl2N3O3
分子量
446.33
储存和溶解度
DMSO:15 mg/mL (33.61 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
