KW-2478|Potent Hsp90 inhibitor, novel, non-ansamycin|CAS# 819812-04-9

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Size	Price	Stock
5mg	$190.00	In stock
10mg	$260.00	In stock
50mg	$680.00	In stock
100mg	$980.00	In stock

Publications citing ApexBio Products

Nature.
2017 Jan 19;541(7637):417-420.

Nature.
2016 Apr 21;532(7599):398-401.

Science.
2016 Aug 5;353(6299)594-8

Nature Biotechnology.
2017 Jun;35(6):569-576

Cell.
2017 Apr 6;169(2):286-300.

Cell.
2015 Aug 27;162(5):987-1002.

Cell.
2015 Feb 12;160(4):729-44.

Nature Medicine.
2017 Apr;23(4):493-500.

Cancer Cell.
2017 May 8;31(5):635-652.e6.

Immunity.
2016 Jan 19;44(1):88-102

Nat Cell Biol.
2015 May;17(5):627-38.

Nat Immunol.
2017 Jun;18(6):654-664.

Nat Neurosci.
2015 Oct;18(10):1464-73.

Cell Res.
2016 Sep;26(9):1007-20.

Mol Cell.
2017 May 18;66(4):546-557.

Mol Cell.
2017 Jun 1;66(5):698-710.

Mol Cell.
2017 Mar 2;65(5):941-955.e8.

Nat Commun.
2016 Feb 1;7:10492.

J Cell Biol.
2016 Apr 11;213(1):109-25.

Cell Host Microbe.
2016 Jul 13;20(1):13-24.

Proc Natl Acad Sci U S A.
2016 Mar 8;113(10):2585-90.

Proc Natl Acad Sci U S A.
2015 Jun 30;112(26):E3365-73.

Proc Natl Acad Sci U S A.
2015 Jul 28;112(30):9412-7.

Autophagy.
2016 Jul 2;12(7):1129-52.

Cancer Res canres.
2946.2015.

Elife.
2016 Jan 14;5. pii: e12203.

Nucleic Acids Res.
2016 Feb 18;44(3):e2.

EMBO Rep.
2015 Sep;16(9):1114-30.

Oncogene.
2016 Mar 21.

Cell Rep.
2015 Sep 29;12(12):1986-96.

Cell Death Differ.
2016 Jun;23(6):1026-37.

Cell Death Differ.
2016 Jan;23(1):76-88.

Quality Control

Quality Control & MSDS

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Purity = 98.00%

Chemical structure

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 > 10 mM	Storage	Store at -20°C
General tips	N/A
Shipping Condition	N/A

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.