ZT-12-037-01 是一种 ATP 竞争性 STK19 抑制剂,对 STK19 (WT) 和 STK19 (D89N) 的 IC50 值分别为 23.96 和 27.94 nM
产品描述
Zt-12-037-01 is a ATP competitive STK19 inhibitor(IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N),respectively).
体外活性
ZT-12-037-01 significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation and proliferation.
体内活性
ZT-12-037-01 as a specific STK19-targeted inhibitor and it effectively blocks oncogenic NRAS-driven melanocyte malignant transformation and melanoma growth in vivo.
动物实验
ZT-12-037-01 (injection subcutaneously; 25-50 mg/kg; once daily; 21 days) inhibits growth of SK-MEL-2 xenograft melanoma and the sections of tumors indicates induction of apoptosis by increasing cleaved caspase-3.
Cas No.
2328073-61-4
分子式
C21H31N5O2
分子量
385.512
储存和溶解度
DMSO:41 mg/mL (106.36 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years