| Identification | Back Directory | [Name]
2H-1-Benzopyran-6-carboxamide, 5-methoxy-N-[3-methoxy-4-[2-(2-piperidinyl)ethoxy]phenyl]-2,2-dimethyl- | [CAS]
2411429-33-7 | [Synonyms]
NCT-58
2H-1-Benzopyran-6-carboxamide, 5-methoxy-N-[3-methoxy-4-[2-(2-piperidinyl)ethoxy]phenyl]-2,2-dimethyl- | [Molecular Formula]
C27H34N2O5 | [MOL File]
2411429-33-7.mol | [Molecular Weight]
466.57 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
12.14±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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.
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| [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. |
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