UC-514321 是NSC370284 的结构类似物,靶向STAT3/5并选择性抑制TET1的表达,且活性更高。它有较低的毒性,在体内外均表现出良好的抗急性髓系白血病活性。
产品描述
UC-514321 directly targets STAT3/5 and represses TET1 expression. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.
体外活性
UC-514321 (0-500 nM, 48 h) inhibits AML cells viability TET1-signaling dependently.UC-514321 increases apoptosis in AML cells not in normal HSPCs.
体内活性
In AML mice models, UC-514321 (2.5 mg/kg, i.p., once per day, for 10 days) exhibits more potent anti-tumor activity than NSC370284.
Cas No.
299420-83-0
分子式
C26H35NO5
分子量
441.56
储存和溶解度
DMSO:25 mg/mL (55.62 mM),Need ultrasonic
H2O:50 mg/mL (113.23 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years