Itraconazole(Synonyms: R51211)

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Itraconazole (Synonyms: R51211) 纯度: 99.15%

Itraconazole (R51211) 是一种三唑类抗真菌药，也是一种有效的口服活性的 Hedgehog 信号通路拮抗剂，IC50 约为 800 nM。Itraconazole 可有效抑制羊毛甾醇 14α-脱甲基酶 (Cytochrome P450) ，从而抑制羊毛甾醇向麦角固醇的氧化转化。Itraconazole 具有抗癌和抗血管生成作用。 Itraconazole 也是一种 oxysterol-binding protein (OSBP) 抑制剂。

Itraconazole(Synonyms: R51211)

Itraconazole Chemical Structure

CAS No. : 84625-61-6

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生物活性

Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor[1][2][3][4].

IC50 & Target

Fungal[1]
IC50: ~800 nM (Hedgehog signaling pathway)[1]
14α-demethylase (cytochrome P450 enzyme)[3]
体外研究
(In Vitro)

Itraconazole has anti-proliferation of HUVEC (IC50 of 0.16 μM)[2].
Itraconazole inhibits endothelial cell cycle progression at the G1 phase in vitro[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.
体内研究
(In Vivo)

Itraconazole (75-100 mg/kg; oral gavage; twice per day; for 18 days; female outbred athymic nude mice) treatment suppresses Hh pathway activity and the growth of medulloblastoma in a mouse allograft model[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 outbred athymic nude mice (6-7-week-old) injected with Ptch+/− cells[1]
Dosage: 75 mg/kg, 100 mg/kg
Administration: Oral gavage; twice per day; for 18 days
Result: Suppressed Hh pathway activity and the growth of medulloblastoma in a mouse allograft model.

Clinical Trial

分子量

705.63

Formula

C35H38Cl2N8O4
CAS 号

84625-61-6
中文名称

伊曲康唑；依他康唑
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 6.25 mg/mL (8.86 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4172 mL 7.0859 mL 14.1717 mL
5 mM 0.2834 mL 1.4172 mL 2.8343 mL
10 mM — — —

*

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 (protect from light)。-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： 0.5% CMC-Na/saline water

    Solubility: 20 mg/mL (28.34 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.62 mg/mL (0.88 mM); Clear solution

    此方案可获得 ≥ 0.62 mg/mL (0.88 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 6.2 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

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 0.62 mg/mL (0.88 mM); Clear solution

    此方案可获得 ≥ 0.62 mg/mL (0.88 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 6.2 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]. Kim, J., et al., Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth. Cancer Cell, 2010. 17(4): p. 388-99.

    [2]. Chong, C.R., et al., Inhibition of angiogenesis by the antifungal drug itraconazole. ACS Chem Biol, 2007. 2(4): p. 263-70.

    [3]. Pace JR, et al. Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic. J Med Chem. 2016 Apr 28;59(8):3635-49.

    [4]. Albulescu L, et al. Uncovering oxysterol-binding protein (OSBP) as a target of the anti-enteroviral compound TTP-8307. Antiviral Res. 2017;140:37-44.

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