KW 2478

An Hsp90 inhibitor

KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).1 It inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin's lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively). KW 2478 decreases expression of the Hsp90 client proteins IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells. In vivo, KW 2478 (100 mg/kg) reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model.

574.7

≥98%

COC1=CC(C(C2=C(CC(N(CCOC)CCOC)=O)C(CC)=C(O)C=C2O)=O)=CC=C1OCCN3CCOCC3

C30H42N2O9

819812-04-9

≥ 4 years

DMF: 5 mg/ml DMSO: 5 mg/ml DMSO:PBS (pH 7.2) (1:7): 0.125 mg/ml Ethanol: insolbule PBS (pH 7.2): insolbule