GPX4-IN-3 (26a) 是有效的谷胱甘肽过氧化物酶4(GPX4)抑制剂,可选择性诱导铁死亡 (ferroptosis)。GPX4-IN-3 (26a) 在1 μM 的浓度可抑制GPX4 71.7% 活性。
生物活性 | GPX4-IN-3 (26a) is a potentglutathione peroxidase4 (GPX4)inhibitor as a selectiveferroptosisinducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM[1]. |
体外研究 (In Vitro) | GPX4-IN-3 (26a) exhibits IC50values of 0.78 μM, 6.9 μM, 0.15 μM and 4.73 μM in 4T1, MCF-7, HT1080 and HT1080 (with Fer-1) cells, respectively[1]. GPX4-IN-3 (26a) exhibits outstanding GPX4 inhibitory activity with a percent inhibition up to 71.7% at 1.0 μM compared to 45.9% of RSL-3[1]. GPX4-IN-3 (26a) could significantly induce lipid peroxide (LPO) increase and effectively induce ferroptosis with satisfactory selectivity[1]. GPX4-IN-3 (26a) is more likely to induce ferroptosis through the accumulation of intracellular peroxides via inhibiting GPX4 activity[1]. GPX4-IN-3 (26a) significantly increased the level of ROS in 4T1 cells, which could also be reversed by Ferrostatin-1 (fer-1)[1].
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体内研究 (In Vivo) | GPX4-IN-3 (26a) exertes antitumor activity and good biological safety in vivo[1].
Animal Model: | Mouse 4T1 xenograft model[1]. | Dosage: | 15 and 30 mg/kg. | Administration: | Intravenous injection, every two days for a total of five times. | Result: | Significantly suppress tumor growth with a tumor growth inhibition (TGI) value of 33.2 and 55.1% at 15 and 30 mg/kg, respectively. |
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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 : 67.5 mg/mL(127.35 mM;Need ultrasonic) 配制储备液 1 mM | 1.8867 mL | 9.4333 mL | 18.8665 mL | 5 mM | 0.3773 mL | 1.8867 mL | 3.7733 mL | 10 mM | 0.1887 mL | 0.9433 mL | 1.8867 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% (20%SBE-β-CDin saline) Solubility: 6.75 mg/mL (12.73 mM); Suspended solution; Need ultrasonic
此方案可获得 6.75 mg/mL (12.73 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 67.5 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。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 6.75 mg/mL (12.73 mM); Clear solution
此方案可获得 ≥ 6.75 mg/mL (12.73 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 67.5 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。 |