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KW-2478

Catalog No. T6558   CAS 819812-04-9
Synonyms: KW2478

KW-2478 is a non-ansamycin HSP90 inhibitor with IC50 of 3.8 nM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
KW-2478 Chemical Structure
KW-2478, CAS 819812-04-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 51.00
2 mg In stock $ 74.00
5 mg In stock $ 122.00
10 mg In stock $ 197.00
25 mg In stock $ 333.00
50 mg In stock $ 497.00
100 mg In stock $ 697.00
1 mL * 10 mM (in DMSO) In stock $ 216.00
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Purity: 98.75%
Purity: 98.68%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description KW-2478 is a non-ansamycin HSP90 inhibitor with IC50 of 3.8 nM.
Targets&IC50 HSP90:3.8 nM
In vitro KW-2478 inhibits the binding of bRD to Hsp90α with IC50 of 3.8 nM. KW-2478 degradates the Hsp90 client proteins, including FGFR3 and IGF-1Rβand c-Raf-1. KW-2478 reduces the level of phosphorylated Erk1/2. KW-2478 induces apoptosis by cleavage of PARP, a substrate of caspase-3 In U266 cells,. KW-2478 has Time dependency of antiproliferative activity, consecutive drug exposure for at least 12 hours is necessary to to exert potent antitumor activity. KW-2478 downregulates the translocation products of IgH locus. KW-2478 inhibits the transcription of c-Maf and cyclin D1 genes by mainly suppressing the function of Cdk9. [1] KW-2478 has potent and broad growth inhibitory activities against various cell lines, KW-2478 inhibites 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. KW-2478 also shows potent growth inhibitory activity in primary CLL and NHL cells with EC50 of 40-170 nM and 200-400 nM, respectively. [2].
In vivo KW-2478 suppresses tumor growth and induces the degradation of client proteins in tumors in NCI-H929 s.c. inoculated model at doses of 100 mg/kg or more. KW-2478 reduces both serum M protein and MM tumor burden in the bone marrow in OPM-2/GFP i.v. inoculated mouse model at doses of 100 mg/kg. [1]
Kinase Assay Hsp90 Binding 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 is added to the wells, and bRD is added to a concentration of 0.1 μmol/L. After removal of solution, poly-HRP streptavidin solution dilutes 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 are added, followed by measurement of absorbance at 450 nm using a microplate spectrophotometer.
Cell Research To measure the IC50, OPM-2/green fluorescent protein (GFP) cells, KMS-11 cells, OPM-2/GFP and other cells are plated into 96-well plates and treat with KW-2478. After 72 hours of cultivation, cell viability is determined using Cell Proliferation Reagent WST-1. WST reagent is added to the wells, followed by incubation for 4 hours at 37 °C. After that, the absorbance at 450 nm with reference at 650 nm is measured with a microplate spectrophotometer. To examine time dependency of antiproliferative activity of KW-2478, the cells are plated into 96-well V-bottomed plates and treated with KW-2478. After 0 hour and at intervals from 3 to 72 hours at 37 °C, the supernatant is aspirated. After drug-free medium is added to the wells, the supernatant is aspirated again. Finally, drug-free medium is added to the wells, and the plates are further incubated for the remainder of the 72-hour period, followed by measurement of cell viabil(Only for Reference)
Synonyms KW2478
Molecular Weight 574.66
Formula C30H42N2O9
CAS No. 819812-04-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 106 mg/mL (184.5 mM)

Ethanol: 3 mg/mL (5.22 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Takayuki Nakashima, et al. Clin Cancer Res, 2010, 16(10), 2792-2802. 2. Juliger S, et al. ASH Annual Meeting and Exposition, 2008. 3. Ishii T, et al. Blood Cancer J, 2012, 2(4), e68.

TargetMolCitations

1. Zeng D, Gao M, Zheng R, et al. The HSP90 inhibitor KW-2478 depletes the malignancy of BCR/ABL and overcomes the imatinib-resistance caused by BCR/ABL amplification. Experimental Hematology & Oncology. 2022, 11(1): 1-14 2. Zeng D, Gao M, Zheng R, et al. The HSP90 inhibitor KW-2478 depletes the malignancy of BCR/ABL and overcomes the imatinib-resistance caused by BCR/ABL amplifcation. Experimental Hematology & Oncology. 2022, 11(1): 1-14 3. Li H J, Wang Q S, Han W, et al. Anti-NSCLC activity in vitro of Hsp90N inhibitor KW-2478 and complex crystal structure determination of Hsp90N-KW-2478. Journal of Structural Biology. 2021, 213(2): 107710.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Apoptosis Compound Library Anti-Aging Compound Library Endoplasmic Reticulum Stress Compound Library Hematonosis Compound Library Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

KW-2478 819812-04-9 Cytoskeletal Signaling Metabolism HSP inhibit KW2478 Heat shock proteins KW 2478 Inhibitor inhibitor

 

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