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

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.

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NMS-E973 Chemical Structure

NMS-E973 Chemical Structure

CAS No. : 1253584-84-7

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of NMS-E973:

NMS-E973 Related Antibodies

Top Publications Citing Use of Products

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • Biological Activity

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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)

Cellular Effect
Cell Line Type Value Description References
A2780 IC50
0.069 μM
Compound: 18, NMS-E973
Antiproliferative activity against human A2780 cells assessed as cell viability after 72 hrs by Cell Titre-Glo assay
Antiproliferative activity against human A2780 cells assessed as cell viability after 72 hrs by Cell Titre-Glo assay
[PMID: 24100158]
BT-474 IC50
0.11 μM
Compound: 18, NMS-E973
Inhibition of Hsp90 in human BT474 cells assessed as degradation of Her2 protein level by immunocytochemistry assay
Inhibition of Hsp90 in human BT474 cells assessed as degradation of Her2 protein level by immunocytochemistry assay
[PMID: 24100158]
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].

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

NMS-E973 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

Off-white to yellow

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (110.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2006 mL 11.0028 mL 22.0056 mL
5 mM 0.4401 mL 2.2006 mL 4.4011 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.50 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2006 mL 11.0028 mL 22.0056 mL 55.0140 mL
5 mM 0.4401 mL 2.2006 mL 4.4011 mL 11.0028 mL
10 mM 0.2201 mL 1.1003 mL 2.2006 mL 5.5014 mL
15 mM 0.1467 mL 0.7335 mL 1.4670 mL 3.6676 mL
20 mM 0.1100 mL 0.5501 mL 1.1003 mL 2.7507 mL
25 mM 0.0880 mL 0.4401 mL 0.8802 mL 2.2006 mL
30 mM 0.0734 mL 0.3668 mL 0.7335 mL 1.8338 mL
40 mM 0.0550 mL 0.2751 mL 0.5501 mL 1.3753 mL
50 mM 0.0440 mL 0.2201 mL 0.4401 mL 1.1003 mL
60 mM 0.0367 mL 0.1834 mL 0.3668 mL 0.9169 mL
80 mM 0.0275 mL 0.1375 mL 0.2751 mL 0.6877 mL
100 mM 0.0220 mL 0.1100 mL 0.2201 mL 0.5501 mL
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NMS-E973 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NMS-E9731253584-84-7HSPHeat shock proteinsHsp90αCarcinomabreastLeukemiaMelanomaNeuroblastomaAdenocarcinomacolonovarycancerInhibitorinhibitorinhibit

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