2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  3. HSP Apoptosis
  4. NCT-58

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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NCT-58 Chemical Structure

NCT-58 Chemical Structure

CAS No. : 2411429-33-7

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Based on 1 publication(s) in Google Scholar

NCT-58 Related Antibodies

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Description

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[1].

IC50 & Target[1]

HSP90

 

Apoptosis

 

Cellular Effect
Cell Line 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]
In Vitro

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.

NCT-58 Related Antibodies

Cell Viability Assay[1]

Cell Line: BT474 and SKBR3 cells
Concentration: 0, 0.1, 0.5, 1, 5, 10, 15, 20 μM
Incubation Time: 72 hours
Result: Significantly reduced cell growth.

Apoptosis Analysis[1]

Cell Line: BT474 and SKBR3 cells
Concentration: 0, 2, 10 μM
Incubation Time: 72 hours
Result: Increased the number of early and late apoptotic cells.

Western Blot Analysis[1]

Cell Line: Trastuzumab-resistant JIMT-1 and MDA-MB-453 cells
Concentration: 0, 2, 10 μM
Incubation Time: 72 hours
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.
In Vivo

NCT-58 (30?mg/kg; i.p.; every other day for 47 days) suppresses Trastuzumab-resistant tumor growth[1].
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.

Animal Model: Trastuzumab-resistant xenograft model (female nude mice; 6 weeks; BALB/c)[1]
Dosage: 30 mg/kg
Administration: i.p.; every other day for 47 days
Result: Significantly reduced tumor growth.
Molecular Weight

466.57

Formula

C27H34N2O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C2OC(C)(C)C=CC2=C1OC)NC3=CC=C(C(OC)=C3)OCCC4NCCCC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1433 mL 10.7165 mL 21.4330 mL
5 mM 0.4287 mL 2.1433 mL 4.2866 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.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.82%

SDS (251 KB)

COA (245 KB) HNMR (262 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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 2.1433 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
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NCT-58 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:

NCT-582411429-33-7NCT58NCT 58HSPApoptosisHeat shock proteinsC-terminaltumorgrowthTrastuzumab-resistantHSP90angiogenesis breast cancerstem-like cellsHER2-positiveInhibitorinhibitorinhibit

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