KW-2478 functions as an Hsp90 inhibitor, displaying an IC50 of 3.8 nM against Hsp90α. It exhibits anti-proliferative effects on multiple myeloma (MM) and non-Hodgkin’s lymphoma (NHL), with GI50 values as follows: 0.30 μM (OPM-2/GFP), 0.34 μM (KMS-11), 0.39 μM (RPMI 8226), 0.12 μM (NCI-H929), 0.36 μM (Raji), 0.098 μM (SR), and 0.33 μM (SC-1). Moreover, KW-2478 impedes the transcription of c-Maf and Cyclin D1 genes primarily through the inhibition of Cdk9 activity [1].
体内研究
KW-2478, administered intravenously at doses ranging from 25 to 200 mg/kg, suppresses tumor growth in SCID mice implanted with NCI-H929 cells, without inducing weight loss. At a dose of 100 mg/kg, intravenously administered KW-2478 leads to the degradation of Hsp90 client proteins (IGF-1Rβ, c-Raf-1, Cdk9) and dephosphorylation of Erk1/2 proteins in NCI-H929 tumors in mice [1].
体外研究
KW-2478 functions as an Hsp90 inhibitor, displaying an IC50 of 3.8 nM against Hsp90α. It exhibits anti-proliferative effects on multiple myeloma (MM) and non-Hodgkin’s lymphoma (NHL), with GI50 values as follows: 0.30 μM (OPM-2/GFP), 0.34 μM (KMS-11), 0.39 μM (RPMI 8226), 0.12 μM (NCI-H929), 0.36 μM (Raji), 0.098 μM (SR), and 0.33 μM (SC-1). Moreover, KW-2478 impedes the transcription of c-Maf and Cyclin D1 genes primarily through the inhibition of Cdk9 activity [1].
搜索
