KW-2478

819812-04-9

C30H42N2O9

DMSO : >= 83.3 mg/mL (144.96 mM)

Metabolic Enzyme/Protease; Cell Cycle/DNA Damage

KW-2478 is an inhibitor of Hsp90alpha, with an IC₅₀ of 3.8 nM, and has antitumor activity against various human hematological tumor cells. IC50 & Target: IC50: 3.8 nM (Hsp90alpha)^[1] In Vitro: KW-2478 is an inhibitor of Hsp90, with an IC₅₀ of 3.8 nM for Hsp90alpha. KW-2478 shows anti-proliferative activity against multiple myeloma (MM) and non-Hodgkin’s lymphoma (NHL), with GI₅₀s of 0.30 uM (OPM-2/GFP), 0.34 uM (KMS-11), 0.39 uM (RPMI 8226), 0.12 uM (NCI-H929), 0.36 uM (Raji), 0.098 uM (SR), and 0.33 uM uM (SC-1). KW-2478 also inhibits the transcription of c-Maf and Cyclin D1 genes by mainly suppressing the function of Cdk9^[1]. In Vivo: KW-2478 (25-200 mg/kg, i.v.) inhibits tumor growth in combined immunodeficiency (SCID) mice bearing NCI-H929 cells, without body weight loss. KW-2478 (100 mg/kg, i.v.) causes degradation of the Hsp90 client proteins (IGF-1Rbeta, c-Raf-1, Cdk9) levels and dephosphorylated Erk1/2 proteins in NCI-H929 tumors of mice^[1].