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KW-2478

SKU: orb1300660

Description

KW-2478 is a potent small molecule inhibitor of HSP90 with an IC50 of 3.8 nM. It is a non-ansamycin compound used in cancer research to study oncogenic client protein degradation in both in vitro and in vivo experimental models.

Research Area

Metabolism Research, Signal Transduction

Images & Validation

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KW-2478

Key Properties

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CAS Number819812-04-9
MW574.66
Purity99.52% (May vary between batches)
FormulaC30H42N2O9
SMILESCCc1c(O)cc(O)c(C(=O)c2ccc(OCCN3CCOCC3)c(OC)c2)c1CC(=O)N(CCOC)CCOC
TargetHSP
SolubilityEthanol:3 mg/mL (5.22 mM);DMSO:106 mg/mL (184.46 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (8.7 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50
HSP90:3.8 nM
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.
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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. 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. .
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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)
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Heat shock proteins, Inhibitor, HSP, HSP90, inhibit, KW 2478, KW2478, KW-2478

Similar Products

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  • KW-2478

    KW-2478 [orb1223043]

    >98% (HPLC)

    819812-04-9

    574.66

    C30H42N2O9

    1 g, 500 mg, 200 mg, 25 mg, 50 mg, 2 mg, 5 mg, 10 mg, 100 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
23116322 ↗

Key Properties

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No computed properties available.

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KW-2478 (orb1300660)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 100.00
2 mg
$ 120.00
5 mg
$ 170.00
10 mg
$ 240.00
1 ml x 10 mM (in DMSO)
$ 260.00
25 mg
$ 380.00
50 mg
$ 540.00
100 mg
$ 740.00
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