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

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.
2018 Mar 29;555(7698):673-677.

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.
2018 Feb 22;172(5):1007-1021.e17.

Cell.
2017 Nov 30;171(6):1284-1300.e21.

Cell.
2017 Aug 17. pii: S0092-8674(17)30869-3.

Cell.
2017 Jul 13;170(2):312-323

Nat Med.
2018 Jan 29.

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.
2018 Mar 12;33(3):401-416.e8.

Cancer Cell.
2017 Aug 14;32(2):253-267.e5.

Cell Stem Cell.
2017 Nov 20. pii: S1934-5909(17)30375-2.

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

Immunity.
2018 Jan 16;48(1):59-74.e5.

Immunity.
2017 Oct 17;47(4):635-647.e6.

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

Nat Cell Biol.
2018 Feb;20(2):186-197.

Nat Cell Biol.
2017 Dec 11.

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

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

Sci Transl Med.
2017 Dec 13;9(420). pii: eaal3765.

Sci Transl Med.
2017 Nov 22;9(417). pii: eaan8462.

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

Cell Host Microbe.
2017 Oct 11;22(4):561-573.e4.

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

Mol Cell.
2017 Nov 16;68(4):731-744.e9.

Mol Cell.
2017 Oct 5;68(1):210-223.e6.

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	≥100mg/mL in DMSO	Storage	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

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.