PQ401

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PQ401  纯度: 99.88%

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)。

PQ401

PQ401 Chemical Structure

CAS No. : 196868-63-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1191 In-stock
10 mg ￥1083 In-stock
50 mg ￥3464 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 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-mediated apoptosis[1].

IC50 & Target

IGF-IR; apoptosis[1]
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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

341.79

Formula

C18H16ClN3O2
CAS 号

196868-63-0
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 : 14.29 mg/mL (41.81 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Gable KL, Maddux BA, Penaranda C, Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth. Mol Cancer Ther. 2006 Apr;5(4):1079-86.

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