An Hsp90 inhibitor (IC50 = 3.8 nM for Hsp90α); inhibits the growth of OPM-2/GFP

KW 2478 – 25 mg

Brand:
Cayman
CAS:
819812-04-9
Storage:
-20
UN-No:
Non-Hazardous - /

KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).{42521} 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.  

 

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Description

An Hsp90 inhibitor (IC50 = 3.8 nM for Hsp90α); 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); decreases expression of IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells; 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 at 100 mg/kg,

Formal name: 2-ethyl-3,5-dihydroxy-N,N-bis(2-methoxyethyl)-6-[3-methoxy-4-[2-(4-morpholinyl)ethoxy]benzoyl]-benzeneacetamide

Synonyms: 

Molecular weight: 574.7

CAS: 819812-04-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Heat Shock Proteins||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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