An HSP90 inhibitor
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NMS-E973

Item No. 22352

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[2,4-dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide
CAS Number
1253584-84-7
Molecular Formula
C22H22N4O7
Formula Weight
454.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/ml
λmax
304 nm
SMILES
OC1=CC(OC2=CC=C([N+]([O-])=O)C=C2)=C(C3=CC(C(NC4CCN(C)CC4)=O)=NO3)C(O)=C1
InChi Code
InChI=1S/C22H22N4O7/c1-25-8-6-13(7-9-25)23-22(29)17-12-20(33-24-17)21-18(28)10-15(27)11-19(21)32-16-4-2-14(3-5-16)26(30)31/h2-5,10-13,27-28H,6-9H2,1H3,(H,23,29)
InChi Key
YLQODGGPIHWTHR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    10 mg

    $283

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    25 mg

    $655

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    Cayman Chemical
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    Product Description

    NMS-E973 is an inhibitor of heat shock protein 90 (HSP90; IC50 = 10 nM in a fluorescence polarization assay).1 It decreases HER2 protein expression (IC50 = 110 nM) in BT474 breast cancer cells and inhibits the growth of a 16 cancer cell line panel (IC50s = 13-362 nM).1,2 NMS-E973 (60 mg/kg, i.v., per day for ten days) reduces tumor growth by 74% in an A2780 xenograft mouse model. It reduces expression of HSP90 client proteins, phosphorylated ERK and AKT, and total AKT in lysates from A2780 tumors. NMS-E973 also completely eradicates MOLM-13 acute myeloid leukemia tumors in a mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brasca, M.G., Mantegani, S., Amboldi, N., et al. Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). Bioorg. Med. Chem. 21(22), 7047-7063 (2013).

    2. Fogliatto, G., Gianellini, L., Brasca, M.G., et al. NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases. Clin. Cancer Res. 19(13), 3520-3532 (2013).