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KW-2478

novel, non-ansamycin, potent Hsp90 inhibitor

KW-2478

Catalog No. A4062
Size Price Stock Qty
5mg $170.00 In stock
10mg $230.00 In stock
50mg $590.00 In stock
100mg $960.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

KW-2478

Biological Activity

Description KW-2478 is a novel, non-ansamycin, potent inhibitor of Hsp90 with IC50 value of 3.8 nM.
Targets Hsp90          
IC50 3.8 nM          

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Chemical Properties

Cas No. 819812-04-9 SDF Download SDF
Synonyms KW2478,KW 2478
Chemical Name 2-[2-ethyl-3,5-dihydroxy-6-[3-methoxy-4-(2-morpholin-4-ylethoxy)benzoyl]phenyl]-N,N-bis(2-methoxyethyl)acetamide
Canonical SMILES CCC1=C(C=C(C(=C1CC(=O)N(CCOC)CCOC)C(=O)C2=CC(=C(C=C2)OCCN3CCOCC3)OC)O)O
Formula C30H42N2O9 M.Wt 574.66
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

KW-2478 is a novel and potent nonansamycin inhibitor of heat shock protein 90 (Hsp90) to overcome the limitations, including low water solubility and hepatotoxicity, of 17-allylamino-17-demethoxygeldanamycin (17-AAG). KW-2478 exerts a strong antitumor activity against multiple myeloma (MM) cells with various chromosormal translocation, in which KW-2478 inhibits cell growth and apoptosis associated with Hsp90 client protein degradation and the decreasing of IgH translocation products including FGFR3, c-Maf and cyclin D1. Recent study results have revealed that KW-2478 is able to deplete Hsp90 client Cdk9 and the phosphorylated 4E-BP1, a transcriptional kinase and a transcription inhibitor respectively, leading to the reduced expression of c-Maf and cyclin D1.

Reference

Nakashima T, Ishii T, Tagaya H, Seike T, Nakagawa H, Kanda Y, Akinaga S, Soga S, Shiotsu Y. New molecular and biological mechanism of antitumor activities of KW-2478, a novel nonansamycin heat shock protein 90 inhibitor, in multiple myeloma cells. Clin Cancer Res. 2010; 16(10): 2792-802.