1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP

KW-2478 

Cat. No.: HY-13468 Purity: >98.0%
Handling Instructions

KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.

For research use only. We do not sell to patients.

KW-2478 Chemical Structure

KW-2478 Chemical Structure

CAS No. : 819812-04-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 240 In-stock
Estimated Time of Arrival: December 31
5 mg USD 190 In-stock
Estimated Time of Arrival: December 31
10 mg USD 290 In-stock
Estimated Time of Arrival: December 31
50 mg USD 860 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.

IC50 & Target[1]

HSP90α

3.8 nM (IC50)

In Vitro

KW-2478 is an inhibitor of Hsp90, with an IC50 of 3.8 nM for Hsp90α. KW-2478 shows anti-proliferative activity against multiple myeloma (MM) and non-Hodgkin’s lymphoma (NHL), with GI50s of 0.30 μM (OPM-2/GFP), 0.34 μM (KMS-11), 0.39 μM (RPMI 8226), 0.12 μM (NCI-H929), 0.36 μM (Raji), 0.098 μM (SR), and 0.33 μM μM (SC-1). KW-2478 also inhibits the transcription of c-Maf and Cyclin D1 genes by mainly suppressing the function of Cdk9[1].

In Vivo

KW-2478 (25-200 mg/kg, i.v.) inhibits tumor growth in combined immunodeficiency (SCID) mice bearing NCI-H929 cells, without body weight loss. KW-2478 (100 mg/kg, i.v.) causes degradation of the Hsp90 client proteins (IGF-1Rβ, c-Raf-1, Cdk9) levels and dephosphorylated Erk1/2 proteins in NCI-H929 tumors of mice[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.3 mg/mL (144.96 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7402 mL 8.7008 mL 17.4016 mL
5 mM 0.3480 mL 1.7402 mL 3.4803 mL
10 mM 0.1740 mL 0.8701 mL 1.7402 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

The cells are plated into 96-well plates and treated with KW-2478. After 72 hours of cultivation, cell viability is determined using 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Severe combined immunodeficient (SCID) mice are intraperitoneally injected with anti-asialo GM1 antibody. The next day, all mice are subcutaneously inoculated with NCI-H929 cells (1×107 cells) suspended in PBS containing 50% of Matrigel. After 10 days, tumor volume is measured using the Antitumor test system II, a computer-operated system including software and instruments. SCID mice with tumors (190 to 290 mm3) are selected. After randomly grouping, saline (vehicle) or KW-2478 is intravenously administered to mice once or twice daily for 5 days. 17-AAG is intravenously administered to mice. Tumor volume is calculated by the Anti-tumor test system II as follows: Tumor volume=DL×DS×DS×1/2. Fourteen days after the initial administration, blood samples of each mouse are obtained, followed by measurement of serum M protein (Ig kappa chain) with Human Kappa-b&f ELISA Quantitation Kit. The statistical analysis is performed using SAS software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

574.66

Formula

C₃₀H₄₂N₂O₉

CAS No.

819812-04-9

SMILES

O=C(N(CCOC)CCOC)CC1=C(C(C2=CC=C(OCCN3CCOCC3)C(OC)=C2)=O)C(O)=CC(O)=C1CC

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
KW-2478
Cat. No.:
HY-13468
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KW-2478

Cat. No.: HY-13468