2H-1-Benzopyran-6-carboxamide, 5-methoxy-N-[3-methoxy-4-[2-(2-piperidinyl)ethoxy]phenyl]-2,2-dimethyl-
- Product Name
- 2H-1-Benzopyran-6-carboxamide, 5-methoxy-N-[3-methoxy-4-[2-(2-piperidinyl)ethoxy]phenyl]-2,2-dimethyl-
- CAS No.
- 2411429-33-7
- Chemical Name
- 2H-1-Benzopyran-6-carboxamide, 5-methoxy-N-[3-methoxy-4-[2-(2-piperidinyl)ethoxy]phenyl]-2,2-dimethyl-
- Synonyms
- NCT-58;NCT-58, 10 mM in DMSO;5-methoxy-N-{3-methoxy-4-[2-(piperidin-2-yl)ethoxy]phenyl}-2,2-dimethyl-2H-chromene-6-carboxamide;2H-1-Benzopyran-6-carboxamide, 5-methoxy-N-[3-methoxy-4-[2-(2-piperidinyl)ethoxy]phenyl]-2,2-dimethyl-
- CBNumber
- CB59974989
- Molecular Formula
- C27H34N2O5
- Formula Weight
- 466.57
- MOL File
- 2411429-33-7.mol
2H-1-Benzopyran-6-carboxamide, 5-methoxy-N-[3-methoxy-4-[2-(2-piperidinyl)ethoxy]phenyl]-2,2-dimethyl- Property
- Boiling point:
- 578.1±50.0 °C(Predicted)
- Density
- 1.152±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 50 mg/mL (107.17 mM; Need ultrasonic)
- pka
- 12.14±0.70(Predicted)
- form
- Solid
- color
- White to off-white
2H-1-Benzopyran-6-carboxamide, 5-methoxy-N-[3-methoxy-4-[2-(2-piperidinyl)ethoxy]phenyl]-2,2-dimethyl- Chemical Properties,Usage,Production
Uses
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].
Biological Activity
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]. 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]. 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].
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].
| 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. |
IC 50
HSP90; Apoptosis
References
[1]. Park S, et al. The C-terminal HSP90 inhibitor NCT-58 kills trastuzumab-resistant breast cancer stem-like cells. Cell Death Discov. 2021;7(1):354.
2H-1-Benzopyran-6-carboxamide, 5-methoxy-N-[3-methoxy-4-[2-(2-piperidinyl)ethoxy]phenyl]-2,2-dimethyl- Preparation Products And Raw materials
Raw materials
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