2411429-33-7
2411429-33-7 structure
- Name: NCT-58
- Chemical Name: NCT-58
- CAS Number: 2411429-33-7
- Molecular Formula: C27H34N2O5
- Molecular Weight: 466.57
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2022-02-21 09:55:32
- Modify Date: 2024-01-11 11:30:49
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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].
| Name | NCT-58 |
|---|
| 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]. |
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| Related Catalog | |
| Target |
HSP90 Apoptosis |
| 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]. 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]. 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. |
| References |
| Molecular Formula | C27H34N2O5 |
|---|---|
| Molecular Weight | 466.57 |
| Storage condition | -20°C |