819812-04-9

Basic information

• Product Name: KW-2478
• Synonyms: KW-2478;2-Ethyl-3,5-dihydroxy-N,N-bis(2-methoxyethyl)-6-[3-methoxy-4-[2-(4-morpholinyl)ethoxy]benzoyl]benzeneacetamide;2-(2-ethyl-3,5-dihydroxy-6-(3-methoxy-4-(2-morpholinoethoxy)benzoyl)phenyl)-N,N-bis(2-methoxyethyl)acetamide;2-Ethyl-3,5-dihydroxy-N,N-bis(2-methoxyethyl)-6-[3-methoxy-4-[2-(4-morpholinyl)ethoxy]benzoyl]benzeneacetamide KW2478;2-(2-Ethyl-3,5-dihydroxy-6-(3-methoxy-4-(2-morpholinoethoxy)benzoyl)phenyl)-N,N-bis(2-methoxye
• CAS NO: 819812-04-9
• Molecular Formula: C30H42N2O9
• Molecular Weight: 574.66248
• Product Categories: Inhibitor
• Mol File: 819812-04-9.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Density: 1.209
• Solubility: ≥100 mg/mL in DMSO
• CAS DataBase Reference: KW-2478(CAS DataBase Reference)
• NIST Chemistry Reference: KW-2478(819812-04-9)
• EPA Substance Registry System: KW-2478(819812-04-9)

Safety Data

• Hazardous Substances Data: 819812-04-9(Hazardous Substances Data)

Usage

Uses

KW-2478 is a novel non-ansamycin potent Hsp90 inhibitor.

Biological Activity

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.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.

Relevant articles and documents

HSP90 FAMILY PROTEIN INHIBITORS

The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): (wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONR7R8 or the like; R2 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or the like; and R4 and R6, which may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like) or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoyl compound or said prodrug.