KW-2478 - CAS 819812-04-9
Catalog number: 819812-04-9
Category: Inhibitor
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KW-2478 is an agent that targets the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Although the mechanism of action remains to be fully elucidated, Hsp90 antagonist KW-2478 appears to inhibit Hsp90, resulting in impaired signal transduction, inhibition of cell proliferation, and the induction of apoptosis in tumor cells. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation or immune responses.
Brife Description:
KW-2478 is a nonansamycin Hsp90 inhibitor with IC50 of 3.8 nM.
Solid powder
DMSO: 115 mg/mL
3 years -20oC powder, 6 months-80oC in solvent.
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Current Developer:
Kyowa Hakko Kirin
1.Anti-tumor activity against multiple myeloma by combination of KW-2478, an Hsp90 inhibitor, with bortezomib.
Ishii T, Seike T, Nakashima T, Juliger S, Maharaj L, Soga S, Akinaga S, Cavenagh J, Joel S, Shiotsu Y. Blood Cancer J. 2012 Apr;2(4):e68. doi: 10.1038/bcj.2012.13. Epub 2012 Apr 27.
Heat shock protein 90 (Hsp90) is a promising target for anti-tumor therapy. We previously reported the anti-tumor activity of a novel Hsp90 inhibitor, KW-2478, in multiple myeloma (MM) as a single agent. In this study, we examined the combinational effect of KW-2478 and bortezomib, a proteasome inhibitor, in vitro and in vivo. In vitro, KW-2478 enhanced bortezomib-induced cell growth inhibition, both in MM cell lines and primary patient MM cells. The combination of KW-2478 and bortezomib also induced caspase activation in MM cell lines. Interestingly, the combination synergistically enhanced the expression of Hsp70B, a homolog of Hsp70, in human MM cells and peripheral blood mononuclear cells, indicating Hsp70B could be a surrogate biomarker for the combination of Hsp90 and proteasome inhibitors. In vivo, the combination of KW-2478 with bortezomib showed synergistic anti-tumor activity without significant body weight loss in a subcutaneously inoculated human myeloma model.
2.New molecular and biological mechanism of antitumor activities of KW-2478, a novel nonansamycin heat shock protein 90 inhibitor, in multiple myeloma cells.
Nakashima T1, Ishii T, Tagaya H, Seike T, Nakagawa H, Kanda Y, Akinaga S, Soga S, Shiotsu Y. Clin Cancer Res. 2010 May 15;16(10):2792-802. doi: 10.1158/1078-0432.CCR-09-3112. Epub 2010 Apr 20.
PURPOSE: The heat shock protein 90 (Hsp90) plays an important role in chaperoning oncogenic client proteins in multiple myeloma (MM) cells, and several Hsp90 inhibitors have shown antitumor activities both in vitro and in vivo. However the precise mechanism of action of Hsp90 inhibitor in MM has not been fully elucidated.
3.Phase I study of KW-2478, a novel Hsp90 inhibitor, in patients with B-cell malignancies.
Yong K1, Cavet J2, Johnson P3, Morgan G4, Williams C5, Nakashima D6, Akinaga S7, Oakervee H8, Cavenagh J8. Br J Cancer. 2016 Jan 12;114(1):7-13. doi: 10.1038/bjc.2015.422. Epub 2015 Dec 22.
BACKGROUND: KW-2478 is a novel, non-ansamycin, non-purine heat-shock protein 90 (Hsp90) inhibitor.
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CAS 819812-04-9 KW-2478

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