KW-2478A novel non-ansamycin potent Hsp90 inhibitor

KW-2478 (CAS 819812-04-9)

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Synonym: 2-(2-ethyl-3,5-dihydroxy-6-(3-methoxy-4-(2-morpholinoethoxy)benzoyl)phenyl)-N,N-bis(2-methoxyethyl)acetamide
Application: A novel non-ansamycin potent Hsp90 inhibitor
CAS Number: 819812-04-9
Molecular Weight: 574.66
Molecular Formula: C30H42N2O9
* Refer to Certificate of Analysis for lot specific data (including water content).
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KW-2478 is a novel, non-ansamycin, potent Hsp90 inhibitor (IC50 of 3.8 nM). KW-2478 is a novel non-purine analogue antagonist for Hsp90. KW-2478 suppresses the binding of bRD to HSP90α in concentration-dependent manner. KW-2478 indicates a potent anti-cancer activity in vitro. KW-2478 clearly prevents cancer cell growth in B-cell lymphoma (EC50 of 101-252), mantle cell lymphoma (EC50 of 81.4-91.4) and multiple myeloma (EC50 of 120-622 nM). KW-2478 also shows potent growth inhibitory activity in primary CLL (EC50 of 40-170 nM) and NHL (EC50 of 200-400 nM) cells. KW-2478 depletes 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 have been 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.


References

PMID: 20406843

Physical State :
Solid
Solubility :
≥115 mg/mL in DMSO <1 mg/mL in Water ≥3 mg/mL in Ethanol
Storage :
Store at -20° C
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
23116322
SMILES :
CCC1=C(C=C(C(=C1CC(=O)N(CCOC)CCOC)C(=O)C2=CC(=C(C=C2)OCCN3CCOCC3)OC)O)O

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Certificate of Analysis

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