Research Area
Product Type
United States ( Change Country )
KW-2478 Chemical Structure
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Biological Activity
KW-2478 is a novel non-ansamycin potent Hsp90 inhibitor with an IC50 of 3.8 nM. KW-2478 is a novel non-purine analogue antagonist for Hsp90. KW-2478 suppressed the binding of bRD to HSP90α in concentration-dependent manner. KW-2478 indicated a potent anti-cancer activity both in vitro and in vivo. KW-2478 clearly prevented cancer cell growth in all cell lines, with EC50 of 101-252, 81.4-91.4 and 120-622 nM for B-cell lymphoma, mantle cell lymphoma and multiple myeloma, respectively. KW-2478 also showd potent growth inhibitory activity in primary CLL (n=3) and NHL (n=2) cells with EC50 of 40-170 nM and 200-400 nM, respectively. KW-2478 depleted the Hsp90 client Cdk9, a transcriptional kinase, and the phosphorylated 4E-BP1, a translational inhibitor. Both inhibitory effects of KW-2478 on such transcriptional and translational pathways were shown to reduce c-Maf and cyclin D1 expression. In NCI-H929 s.c. inoculated model, KW-2478 displayed a significant inhibition of tumor growth and induced the degradation of client proteins in tumors. [1][2]
References on KW-2478
- [1] Clin Cancer Res. 2010 May 15;16(10):2792-802.
- [2] http://ash.confex.com/ash/2008/webprogram/Paper7755.html ;
Chemical Information
| Molecular Weight (WM): | 574.66 |
|---|---|
| Formula: | C30H42N2O9 |
| CAS No.: | 819812-04-9 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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