Quercetagetin (6-Hydroxyquercetin) 是一种类黄酮。Quercetagetin 是一种中等强度和选择性的,细胞渗透性的pim-1激酶抑制,IC50为 0.34 μM。具有抗炎和抗肿瘤活性。
生物活性 | Quercetagetin (6-Hydroxyquercetin) is a flavonoid[1]. Quercetagetin is a moderately potent and selective, cell-permeablepim-1kinase inhibitor (IC50, 0.34 μM)[2]. Anti-inflammatory and anticancer properties. |
IC50& Target[2] | PIM1 0.34 μM (IC50) | PIM2 3.45 μM (IC50) | RSK2 2.82 μM (IC50) | PKA 21.2 μM (IC50) |
|
体外研究 (In Vitro) | Quercetagetin also inhibits PIM2, PKA, and RSK2 with IC50s of 3.45, 21.2, and 2.82 μM, respectively[2]. Quercetagetin (0.1, 1, 10, and 100 μM, 72 hours) inhibits growth of RWPE2 prostate cancer cells with average ED50is 3.8 μM[2].
Cell Viability Assay[2] Cell Line: | RWPE2 prostate cancer cells | Concentration: | 0.1, 1, 10, and 100 μM | Incubation Time: | 72 hours | Result: | Inhibited growth of RWPE2 prostate cancer cells with average ED50is 3.8 μM. |
|
体内研究 (In Vivo) | Quercetagetin significantly inhibits UVB-induced skin cancer development. Topical application of 4 or 20 nmol of Quercetagetin to mouse skin reduces tumor incidence by 32.0% and 46.7%, respectively[3].
Animal Model: | SKH-1 hairless mice model[3] | Dosage: | 4 or 20 nmol | Administration: | Topical application; 28 weeks | Result: | Inhibited UVB-induced skin tumorigenesis in SKH-1 hairless mice models. Delayed the development of tumors and reduced tumor volumes in an SKH-1 hairless mice model. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
中文名称 | |
结构分类 | |
来源 | - Plants
- Eriocaulaceae
- Eriocaulon L.
|
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 |
|
溶解性数据 | In Vitro: DMSO : 125 mg/mL(392.79 mM;Need ultrasonic) 配制储备液 1 mM | 3.1423 mL | 15.7114 mL | 31.4228 mL | 5 mM | 0.6285 mL | 3.1423 mL | 6.2846 mL | 10 mM | 0.3142 mL | 1.5711 mL | 3.1423 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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (6.54 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.54 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.54 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.54 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|