KPT-251 是一种选择性核输出抑制剂。
产品描述
KPT-251 is a selective nuclear export inhibitor.
体外活性
Treatment of Glioblastoma neurosphere cultures with KPT-251 revealed dose-responsive growth inhibition in seven patient-derived GBM lines[1].
体内活性
In a systemic metastasis model, following intracardiac injection of PCb2 cells, 80% (8/10) of controls, 10% (1/10) Selinexor- and 20% (2/10) KPT-251-treated animals developed radiographic evidence of lytic bone lesions. Similarly, after intra-tibial injection, the lytic areas were higher in controls than in Selinexor and KPT-251 groups. Analogously, the serum levels of osteoclast markers (mTRAP and type I collagen fragment, CTX), were significantly higher in controls than in Selinexor- and KPT-251-treated animals. Importantly, overall survival and disease-free survival were significantly higher in Selinexor- and KPT-251-treated animals when compared to controls[2].
Cas No.
1388841-50-6
分子式
C14H7F6N5O
分子量
375.23
别名
KPT251
储存和溶解度
DMSO:65 mg/ml (173.23 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years