mTOR inhibitor-3 是一种mTOR抑制剂,Ki=1.5 nM。在细胞实验及体内药代动力学 (PK)/药效学 (PD) 实验中,它都能够抑制mTORC1和mTORC2。
产品描述
mTOR inhibitor-3 is an inhibitor of remarkably selective mTOR (Ki : 1.5 nM)
体外活性
mTOR inhibitor-3 is an mTOR inhibitsor(Ki of 1.5 nM), 500-fold selectivity over closely related PI3 kinases.?mTOR inhibitor-3 inhibits NCI-PC3 and MCF7neo/Her2 cells proliferation with IC50s of 150 nM and 57 nM, respectively[2].
体内活性
mTOR inhibitor-3 achieves tumor stasis at the highest 200 mg/kg/day dose examined, which appears to also be approaching the limit of tolerability for this molecule. Plasma levels of mTOR inhibitor-3 6 h following oral administration in PC3 tumor-bearing mice along with the fold decreases of phosphorylated mTORC1 and -2 substrates relative to time-matched vehicle controls.?mTOR inhibitor-3 has moderate terminal elimination half-life (t1/2=1.7 h for mouse(1 mg/kg, iv))?[2].
Cas No.
1207358-59-5
分子式
C25H30N8O2
分子量
474.56
储存和溶解度
DMSO:45 mg/mL (94.82 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years