KW-2478 Inhibitor CAS No. 819812-04-9

Cat. No.	Name	Size	Price
KI1211	KW-2478	5 mg	$432
	KW-2478	10 mg	$592
	KW-2478	50 mg	$1552
	KW-2478	200 mg	$4272

Chemical Characteristic

Product Name	KW-2478
CAS No.	819812-04-9
Molecular Weight	574.66
Formula	C₃₀H₄₂N₂O₉
Chemical Name	2-Ethyl-3,5-dihydroxy-N,N-bis(2-methoxyethyl)-6-[3-methoxy-4-[2-(4-morpholinyl)ethoxy]benzoyl]benzeneacetamide
Smiles	c1(c(c(cc(c1C(=O)c1cc(c(cc1)OCCN1CCOCC1)OC)O)O)CC)CC(=O)N(CCOC)CCOC
Chemical Structure

Biological activities

KW-2478 is a novel heat shock protein 90 (Hsp90) inhibitor. KW-2478 inhibits the binding of bRD to Hsp90α, with an IC50 of 3.8 nM. KW-2478 inhibits human MM cells OPM-2/GFP, KMS-11, RPMI 8226, and NCI-H929 with IC50 of 0.30, 0.34, 0.39, and 0.12 µM, respectively. KW-2478 also inhibits human non-Hodgkin's lymphoma cells Raji, SR and SC-1 with IC50 of 0.36, 0.098, and 0.33 µM, respectively. In vitro, KW-2478 can inhibit growth and induce apoptosis in MM cells. ^[1] The combination of KW-2478 and bortezomib also induces caspase activation in MM cell lines. ^[2] In NCI-H929 s.c. inoculated model, KW-2478 shows a significant suppression of tumor growth and induces the degradation of proteins in tumors. ^[1] In vivo, the combination of KW-2478 with bortezomib shows synergistic anti-tumor activity without significant body weight loss in a subcutaneously inoculated human myeloma model. Furthermore, the combination also shows synergistic reduction of tumor burden in bone marrow in an orthotopic myeloma model. ^[2]

Protocols

For in vitro use, KW-2478 is dissolved in DMSO and diluted in culture medium. For in vivo use, KW-2478 is dissolved in saline. ^[2]

References

[1] Nakashima T, et al. 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): 2792-2802 [2] Ishii T, et al. Anti-tumor activity against multiple myeloma by combination of KW-2478, an Hsp90 inhibitor, with bortezomib. Blood Cancer J. 2012, 2(4): e68.

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