NMS-E973
Based on 2 publication(s) in Google Scholar
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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- Pureté: 99.61%
- CAS No.: 1253584-84-7
- Formule: C22H22N4O7
- Masse moléculaire:454.43
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) NMS-E973
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Activité biologique
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HSP90α 10 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
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| A2780 | IC50 |
0.069 μM
Compound: 18, NMS-E973
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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
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[PMID: 24100158] |
| BT-474 | IC50 |
0.11 μM
Compound: 18, NMS-E973
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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
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[PMID: 24100158] |
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.
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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
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Concentration:
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Incubation Time:24, 48, 72 hours
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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.
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.
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Animal Model:Balb/c male nude mice (aged 6 to 8 weeks) xenografted with the A375 tumors[1]
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Dosage:60 mg/kg
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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).
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Result:Both schedules resulted in tumor shrinkage and TGI of 74% and 89%, respectively.
Chemical Information
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CAS No. 1253584-84-7
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Appearance Solid
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Masse moléculaire 454.43
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Formule C22H22N4O7
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Color Off-white to yellow
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SMILES
O=C(C1=NOC(C2=C(OC3=CC=C([N+]([O-])=O)C=C3)C=C(O)C=C2O)=C1)NC4CCN(C)CC4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Theranostics
2019 Jan 1;9(2):554-572. PMID: 30809293 -
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (536 KB)
- English - EN (536 KB)
- Français - FR (536 KB)
- Deutsch - DE (536 KB)
- Norwegian - NO (536 KB)
- Español - ES (536 KB)
- Swedish - SV (536 KB)
- Italian - IT (536 KB)
- Korean - KR (536 KB)
- Portuguese - PT (536 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| 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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