For research use only.

Catalog No.S7282

7 publications

NMS-E973 Chemical Structure

CAS No. 1253584-84-7

NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases.

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Selleck's NMS-E973 has been cited by 7 publications

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  • (D) Representative images of paraffin-embedded tumor sections were analyzed by active caspase-3 staining. (E) Representative images of paraffin-embedded tumor sections analyzed by TUNEL staining.

    Onco Targets Ther, 2018, 11:1583-1593. NMS-E973 purchased from Selleck.

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Biological Activity

Description NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases.
HSP90 [1]
<10 nM(DC50)
In vitro

NMS-E973 shows a widespread antiproliferative activity with an average IC50 of 1.6 μM, and induces the degradation of client protein, such as Flt3, B-Raf, AKT, which further blocks tumor-related pathways, such as the Raf/MAPK, PI3K/AKT, and JAK/STAT pathways. [1]

Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 29593424     

(A) U87 and (B) SW1088 cells were treated with NMS-E973 for 72 hours. Cell viability was measured by MTT assay. 

Western blot
PUMA / NOXA / BID / BAD / Bak / Bmf ; 

PubMed: 29593424     

(C) The mRNA levels of the indicated gene in SW1088 cells were evaluated by the RT-PCR. (D) Expression of the indicated protein in SW1088 cells was measured by Western blot.

In vivo NMS-E973 (10 mg/kg i.v.) shows a favorable pharmacokinetic profile with selective retention in tumor tissue and ability to cross the BBB. NMS-E973 (60 mg/kg i.v.) shows high antitumor efficacy in all the models tested, including A375 and A2780 xenografts. In addition, NMS-E973 (10 mg/kg i.v.) together with B-Raf inhibitor PLX-4720 at 100 mg/kg produces a synergic anti-tumor effect. [1] In a mouse model of human ovarian cancer, NMS-E973 produces the antitumor activity by inhibition of Hsp90. [2]


Kinase Assay:[1]
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Hsp90 binding assays:

For competition experiments, a protein concentration of 5 nM for Hsp90 and of 200 nM for Trap1 are mixed with 0.5 nmol/L probe (final concentrations). After incubation, the dimethyl sulfoxide (DMSO) compound solution is added to the mixture. The plate is incubated for 18 hours at room temperature and then the fluorescence polarization signal was measured. Data are fitted with the program Dynafit version 3.28.039 or SigmaPlot (SSI) using the mathematical equation for competitive binding of 2 ligands to the receptor.
Animal Research:[1]
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  • Animal Models: Mice bearing A375 xenografts, A2780 xenografts, MOLM-13 xenografts or RKO xenografts.
  • Dosages: ~60 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL warmed (198.05 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 454.43


CAS No. 1253584-84-7
Storage powder
in solvent
Synonyms N/A
Smiles CN1CCC(CC1)NC(=O)C2=NOC(=C2)C3=C(C=C(C=C3OC4=CC=C(C=C4)[N+](=O)[O-])O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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HSP (HSP90) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID