Icaritin(Synonyms: Anhydroicaritin)

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Icaritin (Synonyms: Anhydroicaritin) 纯度: 99.27%

Icaritin (Anhydroicaritin) 是 Epimedium Genusis 的异戊二烯类黄酮衍生物，有效抑制 K562 细胞 (IC50 为 8 µM) 和原代 CML 细胞 (对 CML-CP 的 IC50 值为 13.4 µM，对 CML-BC 的 IC50 值为 18 µM) 的增殖。Icaritin 可以调节 MAPK/ERK/JNK 和 JAK2/STAT3/AKT 信号传导，并具有增强成骨的作用。

Icaritin(Synonyms: Anhydroicaritin)

Icaritin Chemical Structure

CAS No. : 118525-40-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660 In-stock
5 mg ￥600 In-stock
10 mg ￥1100 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium Genusis and potently inhibits proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis[1][2][3.

体外研究
(In Vitro)

Icaritin (4-64 µM; 48 hours; K562, imatinib-resistant cells and primary CML cells) treatment inhibits proliferation of K562, imatinib-resistant cells and primary CML cells [1].
Icaritin (0-64 µM; 48 hours; K562 and primary cells) treatment induces K562 or primary cells apoptosis in an concentration dependent manner[1].
Icaritin (32 µM; K562 cells) treatment increases cell population in the sub-G1 phase in K562 cells[1].
Icaritin (0-64 µM; 48 hours; K562 cells) treatment inhibits MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression. Icaritin treatment also significantly inhibits Bcl-2 protein expression and up-regulated Bax protein expression in K562 with a dose-dependent manner accompanied by the cleavage activation of caspase-3 or caspase-9, and a down-regulated expression of Apaf-1[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.

Cell Proliferation Assay[1]

Cell Line: K562, imatinib-resistant cells and primary CML cells
Concentration: 4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time: 48 hours
Result: Inhibited cell proliferation.

Apoptosis Analysis[1]

Cell Line: K562 or primary cells
Concentration: 0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time: 48 hours
Result: Induced K562 or primary cells apoptosis.

Cell Cycle Analysis[1]

Cell Line: K562 cells
Concentration: 32 µM
Incubation Time:
Result: Cell population in the sub-G1 phase was increased.

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time: 48 hours
Result: Inhibited MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression.

体内研究
(In Vivo)

Icaritin (4-8 mg/kg; intraperitoneal injection; daily; for 10 weeks; female NOD-SCID nude mice) treatment could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow in mouse leukemia 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 NOD-SCID nude mice (6-8 weeks old) with K562 cells[1]
Dosage: 4 mg/kg and 8 mg/kg
Administration: Intraperitoneal injection; daily; for 10 weeks
Result: Could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow.

Clinical Trial

分子量

368.38

Formula

C21H20O6
CAS 号

118525-40-9
中文名称

去水淫羊藿黄素；三七淫羊藿素
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 : 15.62 mg/mL (42.40 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7146 mL 13.5729 mL 27.1459 mL
5 mM 0.5429 mL 2.7146 mL 5.4292 mL
10 mM 0.2715 mL 1.3573 mL 2.7146 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: ≥ 1.56 mg/mL (4.23 mM); Clear solution

    此方案可获得 ≥ 1.56 mg/mL (4.23 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 15.6 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： 50% PEG300    50% saline

    Solubility: 1.51 mg/mL (4.10 mM); Suspended solution; Need ultrasonic

*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]. Zhu Jf, et al. Icaritin shows potent anti-leukemia activity on chronic myeloid leukemia in vitro and in vivo by regulating MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings. PLoS One. 2011;6(8):e23720.

    [2]. Yao D, et al. Icaritin, an exogenous phytomolecule, enhances osteogenesis but not angiogenesis–an in vitro efficacy study. PLoS One. 2012;7(8):e41264.

    [3]. Guo Y, et al. An anticancer agent icaritin induces sustained activation of the extracellular signal-regulated kinase (ERK) pathway and inhibits growth of breast cancer cells. Eur J Pharmacol. 2011 May 11;658(2-3):114-22.

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