An Hsp90 inhibitor
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KW 2478

Item No. 22418

Technical Information
Formal Name
2-ethyl-3,5-dihydroxy-N,N-bis(2-methoxyethyl)-6-[3-methoxy-4-[2-(4-morpholinyl)ethoxy]benzoyl]-benzeneacetamide
CAS Number
819812-04-9
Molecular Formula
C30H42N2O9
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 5 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2) (1:7): 0.125 mg/ml
λmax
229, 281, 313 nm
SMILES
COC1=CC(C(C2=C(CC(N(CCOC)CCOC)=O)C(CC)=C(O)C=C2O)=O)=CC=C1OCCN3CCOCC3
InChi Code
InChI=1S/C30H42N2O9/c1-5-22-23(19-28(35)32(11-13-37-2)12-14-38-3)29(25(34)20-24(22)33)30(36)21-6-7-26(27(18-21)39-4)41-17-10-31-8-15-40-16-9-31/h6-7,18,20,33-34H,5,8-17,19H2,1-4H3
InChi Key
VFUXSYAXEKYYMB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).1 It inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin's lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively). KW 2478 decreases expression of the Hsp90 client proteins IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells. In vivo, KW 2478 (100 mg/kg) reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nakashima, T., Ishii, T., Tagaya, H., et alNew 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. 16(10), 2792-2802 (2010).