SPP-86 是有效的、选择性的RET 酪氨酸激酶抑制剂，其IC50=8 nM。它能够抑制 MCF7 细胞中 RET 诱导激活的 PI3K/Akt 和 MAPK 信号通路，也能抑制 RET 诱导的 ERα 磷酸化。
产品描述
SPP-86 is an effective and selective cell-permeable inhibitor of RET tyrosine kinase with an IC50 of 8 nM.
体外活性
Administration of SPP-86 (0-10 μM) suppresses RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling and estrogen receptorα (ERα) phosphorylation in MCF7 cells. Administration of SPP-86 (0-10 μM) also supppresses MAPK signaling and proliferation in RET/PTC1 expressing TPC1 compared to 8505C or C643 cells [1].
Cas No.
1357349-91-7
分子式
C16H15N5
分子量
277.32
储存和溶解度
DMSO:100 mg/mL (360.59 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
