NCT-58是HSP90C末端的有效抑制剂。NCT-58 不诱导热休克反应 (HSR)，因为它靶向 C 末端区域，并通过同时下调 HER 家族成员以及抑制 Akt 磷酸化来引发抗肿瘤活性。NCT-58 可杀死曲妥珠单抗耐药 (Trastuzumab-resistant) 的乳腺癌干细胞样细胞。NCT-58 诱导 HER2 阳性乳腺癌细胞凋亡。在抗曲妥珠单抗异种移植模型中，NCT-58 可抑制生长和血管生成。
| 生物活性 | NCT-58 is a potent inhibitor of C-terminalHSP90. 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 ofAktphosphorylation. NCT-58 kills Trastuzumab-resistant breastcancerstem-like cells. NCT-58 inducesapoptosisin HER2-positive breastcancercells[1]. |
| IC50& Target[1] | |
体外研究
(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. |
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体内研究
(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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(107.17 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1433 mL | 10.7165 mL | 21.4330 mL | | 5 mM | 0.4287 mL | 2.1433 mL | 4.2866 mL | | 10 mM | 0.2143 mL | 1.0717 mL | 2.1433 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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