MeTC7 是一种维生素 D 受体(VDR)拮抗剂。MeTC7 具有有效的 VDR 抑制活性，IC50值为 2.9 μM。MeTC7 显示出良好的抗肿瘤作用。
| 生物活性 | MeTC7 is aVitamin-D receptor (VDR)antagonist. MeTC7 has potent VDR inhibition activity with anIC50value of 2.9 μM. MeTC7 shows good antitumor effects[1]. |
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体外研究
(In Vitro) | MeTC7 (compound 5) shows potent VDR inhibition activity with an IC50value of 2.9 μM[1].
MeTC7 disrupts the VDR-Ligand-binding domain in Silico[1].
MeTC7 (250 nM; 18 h) suppresses RXRα and Importin-4 expressions in the ovarian cancer cell-line[1].
MeTC7 (250 nM; 18 h) inhibits the viability of ovarian cancer cells and induces PARP1 cleavage[1].
Western Blot Analysis[1] | Cell Line: | 2008 cells | | Concentration: | 250 nM | | Incubation Time: | 18, 12 h | | Result: | Reduced the expression of RXR-α, Importin-4 and increased cleaved PARP1 expression in 2008 cells. |
Cell Viability Assay[1] | Cell Line: | SKOV-3, IGROV-1, CAOV-3, OVCAR-3, OVCAR-8, and 2008 ovarian cancer cell-lines | | Concentration: | 0, 0.25, 0.5, 0.75, 1.0, 1.25 μM | | Incubation Time: | 24 h | | Result: | Reduced the viability of SKOV-3, IGROV-1, CAOV-3, OVCAR-3, OVCAR-8, and 2008 ovarian cancer cell-lines. |
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体内研究
(In Vivo) | MeTC7 (compound 5) (i.p.; 10 mg/kg) reduces the growth of the spontaneous transgenic TH-MYCN neuroblastoma and xenografts in vivo[1].
| Animal Model: | Mice[1] | | Dosage: | 10 mg/kg | | Administration: | IP | | Result: | Reduced the growth of xenografts derived from ovarian cancer, medulloblastoma, and pancreatic cancer cells.
Inhibited the growth of neuroblastoma cells and Xenografts.
Reduced MYCN expression and blocked the growth of TH-MYCN transgene-driven spontaneous neuroblastoma. |
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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 : 16.67 mg/mL(26.95 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 1.6164 mL | 8.0821 mL | 16.1642 mL | | 5 mM | 0.3233 mL | 1.6164 mL | 3.2328 mL | | 10 mM | 0.1616 mL | 0.8082 mL | 1.6164 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1.67 mg/mL (2.70 mM); Clear solution
此方案可获得 ≥ 1.67 mg/mL (2.70 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
