Name: KW-2478
Brand: Selleck Chemicals
SKU: S2685
Rating: 5 (2 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Akt Wnt/beta-catenin PKC ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK Kinesin
Other HSP Inhibitors	Tanespimycin (17-AAG) Elesclomol (STA-4783) Luminespib (NVP-AUY922) Ganetespib (STA-9090) Alvespimycin (17-DMAG) Hydrochloride VER-155008 Onalespib (AT13387) BIIB021 Zelavespib (PU-H71) HSP990 (NVP-HSP990)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
TC32	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
SK-N-SH	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
RD	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
Rh41	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	574.66	Formula	C₃₀H₄₂N₂O₉	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	819812-04-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCC1=C(C(=C(C=C1O)O)C(=O)C2=CC(=C(C=C2)OCCN3CCOCC3)OC)CC(=O)N(CCOC)CCOC

Solubility

In vitro
Batch:

DMSO : 115 mg/mL (200.11 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (17.40mM)	Taking the 1 mL working solution as an example, add 300 μL of 33.33 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	HSP90 3.8 nM
In vitro	KW-2478 inhibits the binding of bRD to Hsp90α with IC50 of 3.8 nM. This compound degrades Hsp90 client proteins, including FGFR3 and IGF-1Rβ and c-Raf-1. It reduces the level of phosphorylated Erk1/2. This chemical induces apoptosis by cleavage of PARP, a substrate of caspase-3, in U266 cells. It has time dependency of antiproliferative activity; consecutive drug exposure for at least 12 hours is necessary to exert potent antitumor activity. This agent downregulates the translocation products of the IgH locus. It inhibits the transcription of c-Maf and cyclin D1 genes by mainly suppressing the function of Cdk9. This compound has potent and broad growth inhibitory activities against various cell lines; it inhibits cancer cell growth in all cell lines, with EC50 of 101-252 nM, 81.4-91.4 nM and 120-622 nM for B-cell lymphoma, mantle cell lymphoma and multiple myeloma, respectively. It also shows potent growth inhibitory activity in primary CLL and NHL cells with EC50 of 40-170 nM and 200-400 nM, respectively. .
Kinase Assay	Hsp90 Binding Assay
Kinase Assay	Human Hsp90α solution (0.5 μg/mL) is fixed on 96-well plates, followed by blocking with TBS containing 1% bovine serum albumin. KW-2478 solutions are added to the wells, and bRD is added to a concentration of 0.1 μmol/L. After removal of solution, poly-HRP streptavidin solution diluted with poly-HRP dilution buffer is added to the wells. After removal of solution, equal volumes of TMB peroxidase substrate and peroxidase solution B are added to the wells. To stop the HRP reaction, 2 mol/L H₂SO₄ is added, followed by measurement of absorbance at 450 nm using a microplate spectrophotometer.
In vivo	KW-2478 suppresses tumour growth and induces the degradation of client proteins in tumours in the NCI-H929 s.c. inoculated model at doses of 100 mg/kg or more. This compound reduces both serum M protein and MM tumour burden in the bone marrow in the OPM-2/GFP i.v. inoculated mouse model at doses of 100 mg/kg.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20406843/ [2] http://ash.confex.com/ash/2008/webprogram/Paper7755.html [3] http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3346683

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KW-2478 HSP inhibitor

Chemical Structure

Molecular Weight: 574.66