PQ401 是一种有效的IGF-IR抑制剂。在 MCF-7 细胞中,PQ401 抑制 IGF-I 刺激的 IGF-IR 自磷酸化,IC50为 12.0 μM。PQ401 可有效抑制 IGF-I 刺激的 MCF-7 细胞生长 (IC50为 6 μM)。PQ401 有潜力用于乳腺癌和其他对 IGF-I 敏感的癌症的研究。PQ401 诱导 caspase 介导的细胞凋亡 (apoptosis)。
生物活性 | PQ401 is a potent inhibitor ofIGF-IRsignaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediatedapoptosis[1]. |
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体外研究 (In Vitro) | PQ401 (1, 5, 10, 25, and 50 μM; 3 days) inhibits proliferation of cultured MCF-7 cells grown in serum or IGF-I in MCF-7 cells[1]. Twenty-four hours of treatment with 15 μM PQ401 induces caspase-mediated apoptosis[1]. PQ401 inhibits autophosphorylation of the IGF-IR kinase domain at concentrations<100 nm, with an ic50<1 μM.
Cell Proliferation Assay[1] Cell Line: | Breast cancer cells, MCF-7 cells | Concentration: | 1, 5, 10, 25, and 50 μM | Incubation Time: | 3 days | Result: | Significantly reduced proliferation (IC50, 8 μM) at concentrations in the range of 1 μM. Produced a dramatic reduction in cell number from pretreatment levels at concentrations >10 μM. |
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体内研究 (In Vivo) | PQ401 (50 or 100 mg/kg; i.p.; thrice a week) results in a significant dose-dependent reduction in tumor growth over the course of the study. PQ401 reduces the growth rate of MCNeuA cells implanted into mice[1].
Animal Model: | Female mice were MCNeuA tumor cells[1] | Dosage: | 50 or 100 mg/kg | Administration: | Administered i.p. thrice a week; 24 days | Result: | Resulted in a significant dose-dependent reduction in tumor growth. Tumor growth in the animals treated with 100 mg/kg was 20% of that in the vehicle-treated controls. This dosing protocol was well tolerated by the animals. |
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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 : 14.29 mg/mL(41.81 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) 配制储备液 1 mM | 2.9258 mL | 14.6289 mL | 29.2577 mL | 5 mM | 0.5852 mL | 2.9258 mL | 5.8515 mL | 10 mM | 0.2926 mL | 1.4629 mL | 2.9258 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: ≥ 1.43 mg/mL (4.18 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (4.18 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 14.3 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: 1.43 mg/mL (4.18 mM); Suspended solution; Need ultrasonic
此方案可获得 1.43 mg/mL (4.18 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 14.3 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1.43 mg/mL (4.18 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (4.18 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 14.3 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。
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