1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP
  3. NMS-E973

NMS-E973 

Cat. No.: HY-17547
Handling Instructions

NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.

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

NMS-E973 Chemical Structure

NMS-E973 Chemical Structure

CAS No. : 1253584-84-7

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Estimated Time of Arrival: December 31
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Description

NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy[1].

IC50 & Target[1]

HSP90α

10 nM (DC50)

In Vitro

NMS-E973 inhibits cancer cell proliferation. NMS-E973 shows a widespread antiproliferative activity, with an average IC50 of 1.6 μM and 15 cell lines with an IC50 <100 nM[1].

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

Cell Proliferation Assay[1]

Cell Line: Carcinoma breast DU-4475, EVSA-T, CAL-51, HCC1954, BT-474, HCC1419, HDQ-P1 cells; Leukemia MV-4-11 and MOLM-13 cells; Melanoma A-375 cells
Concentration:
Incubation Time: 24, 48, 72 hours
Result: IC50s of 13, 16, 56, 61, 73, 76, and 89 nM for DU-4475, EVSA-T, CAL-51, HCC1954, BT-474, HCC1419, HDQ-P1 cells, respectively.
IC50s of 29 and 35 nM for MV-4-11, MOLM-13 cells, respectively.
The IC50 of 133 nM for A-375 cell.
In Vivo

NMS-E973 (60 mg/kg; i.v.) inhibits the growth of A375 tumors subcutaneously or intracranially implanted in mice[1].
NMS-E973 exhibits moderate elimination half-lives (5.55±1.07 h) due to high plasma clearance (39.9±1.70 mL/min/kg) combined with large volumes of distribution (5.83±3.18 L/kg) following intravenous administration (10 mg/kg) in mice[1].

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

Animal Model: Balb/c male nude mice (aged 6 to 8 weeks) xenografted with the A375 tumors[1]
Dosage: 60 mg/kg
Administration: Administered twice daily i.v. according to 2 schedules: (i) every other day for 12 days and (ii) 3 days on/1 day off/3 days on (3-1-3, one cycle).
Result: Both schedules resulted in tumor shrinkage and TGI of 74% and 89%, respectively.
Molecular Weight

454.43

Formula

C₂₂H₂₂N₄O₇

CAS No.

1253584-84-7

SMILES

O=C(C1=NOC(C2=C(OC3=CC=C([N+]([O-])=O)C=C3)C=C(O)C=C2O)=C1)NC4CCN(C)CC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

NMS-E973HSPHeat shock proteinsHsp90αCarcinomabreastLeukemiaMelanomaNeuroblastomaAdenocarcinomacolonovarycancerInhibitorinhibitorinhibit

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NMS-E973
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