NCT-58
Based on 1 Customer Validation
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells.
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- Pureté: 99.63%
- CAS No.: 2411429-33-7
- Formule: C27H34N2O5
- Masse moléculaire:466.57
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
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HSP90 |
Apoptosis |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | IC50 |
8.53 μM
Compound: 80
|
Cytotoxicity against human BT-474 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human BT-474 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 32738983] |
| JIMT-1 | IC50 |
4.45 μM
Compound: 80
|
Cytotoxicity against human JIMT-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human JIMT-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 32738983] |
| SK-BR-3 | IC50 |
2 μM
Compound: 27; NCT-58
|
Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS proliferation assay
Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS proliferation assay
|
[PMID: 36549397] |
NCT-58 treatment (0.1-20 μM; 72 hours) dose-dependently reduces cell viability in HER2-positive BT474 and SKBR3 cells[1].
NCT-58 treatment (0.1-10 μM; 72 hours) increases the number of early and late apoptotic cells in HER2-positive BT474 and SKBR3 cells[1].
NCT-58 treatment (2-10 μM; 72 hours) effectively reduced the levels of truncated p95HER2 and its phosphorylated form, as well as downregulation of Akt and phospho-Akt (Ser473) protein contents in JIMT-1 and MDA-MB-453 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT474 and SKBR3 cells
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Concentration:0, 0.1, 0.5, 1, 5, 10, 15, 20 μM
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Incubation Time:72 hours
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Result:Significantly reduced cell growth.
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Cell Line:BT474 and SKBR3 cells
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Concentration:0, 2, 10 μM
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Incubation Time:72 hours
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Result:Increased the number of early and late apoptotic cells.
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Cell Line:Trastuzumab-resistant JIMT-1 and MDA-MB-453 cells
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Concentration:0, 2, 10 μM
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Incubation Time:72 hours
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Result:Effectively reduced the levels of truncated p95HER2 and its phosphorylated form, as well as downregulation of Akt and phospho-Akt (Ser473) protein contents in JIMT-1 and MDA-MB-453 cells.
NCT-58 (30 mg/kg; i.p.; every other day for 47 days) causes a significant impediment of tumor growth and a marked decrease in tumor weight[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Trastuzumab-resistant xenograft model (female nude mice; 6 weeks; BALB/c)[1]
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Dosage:30 mg/kg
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Administration:i.p.; every other day for 47 days
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Result:Significantly reduced tumor growth.
Chemical Information
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CAS No. 2411429-33-7
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Appearance Solid
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Masse moléculaire 466.57
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Formule C27H34N2O5
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Color White to off-white
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SMILES
O=C(C1=CC=C2OC(C)(C)C=CC2=C1OC)NC3=CC=C(C(OC)=C3)OCCC4NCCCC4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 50 mg/mL (107.17 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)
Pureté et documentation
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Fiche technique (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1433 mL | 10.7165 mL | 21.4330 mL | 53.5825 mL |
| 5 mM | 0.4287 mL | 2.1433 mL | 4.2866 mL | 10.7165 mL | |
| 10 mM | 0.2143 mL | 1.0717 mL | 2.1433 mL | 5.3583 mL | |
| 15 mM | 0.1429 mL | 0.7144 mL | 1.4289 mL | 3.5722 mL | |
| 20 mM | 0.1072 mL | 0.5358 mL | 1.0717 mL | 2.6791 mL | |
| 25 mM | 0.0857 mL | 0.4287 mL | 0.8573 mL | 2.1433 mL | |
| 30 mM | 0.0714 mL | 0.3572 mL | 0.7144 mL | 1.7861 mL | |
| 40 mM | 0.0536 mL | 0.2679 mL | 0.5358 mL | 1.3396 mL | |
| 50 mM | 0.0429 mL | 0.2143 mL | 0.4287 mL | 1.0717 mL | |
| 60 mM | 0.0357 mL | 0.1786 mL | 0.3572 mL | 0.8930 mL | |
| 80 mM | 0.0268 mL | 0.1340 mL | 0.2679 mL | 0.6698 mL | |
| 100 mM | 0.0214 mL | 0.1072 mL | 0.2143 mL | 0.5358 mL |