1. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Apoptosis
  2. Src Akt Apoptosis
  3. Chrysotoxine

Chrysotoxine 是 SrcAkt 的双重抑制剂。Chrysotoxine 通过下调 Src/Akt 信号通路来抑制癌症干细胞 (CSCs) 表型。Chrysotoxine 降低 H460 和 H23 的细胞活力,增加细胞凋亡 (apoptosis) 水平,而对非肿瘤细胞系无作用。Chrysotoxine 在大鼠中显示出快速排泄和低生物利用度的特点。Chrysotoxine 可用于癌症研究。

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Chrysotoxine Chemical Structure

Chrysotoxine Chemical Structure

CAS No. : 156951-82-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
NCI-H460 IC50
127.34 μM
Compound: 3
Cytotoxicity against human NCI-H460 cells assessed as cell viability by MTT assay
Cytotoxicity against human NCI-H460 cells assessed as cell viability by MTT assay
[PMID: 32711292]
体外研究
(In Vitro)

Chrysotoxine (50 nM,24 小时) 降低了 H460 和 H23 的细胞活力,增加了细胞凋亡水平[1]
Chrysotoxine (5-20 nM,72 小时) 抑制了 H460 和 H23 细胞中的 CSC 群体[1]
Chrysotoxine (0-20 nM,过夜) 通过抑制 Src-Akt 活化机制来降低 H460 和 H23 细胞的干性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: 460, H23 cells
Concentration: 0-20 µM
Incubation Time: Overnight
Result: Significant decreased the p-Src and p-Akt expression in a dose-dependent manner instead of Src and Akt.
Significantly reduced the down-stream stem cell transcription factor Sox2 as the decline of p-Src in H460 and H23 cells.

Cell Viability Assay[1]

Cell Line: 460, H23 cells
Concentration: 0, 1, 5, 10, 20 and 50 µM
Incubation Time: 24 h
Result: Significantly reduced cell viability and increased H460 and H23 cells cell apoptosis at 50 µM with IC50s of 127.34 and 145.47 µM, respectively.
Showed no cytotoxic effect on non-tumor cell lines at all tested concentrations.

Cell Differentiation Assay[1]

Cell Line: 460, H23 cells
Concentration: 5-20 µM
Incubation Time: 72 h
Result: Decreased approximately 30, 60, 90 and 95% of the H460 CSC spheroid size at day 7 with treated 1, 5,10 and 20 µM Chrysotoxine, respectively.
Decreased approximately 40, 60, 80 and 92% of the H23 CSC spheroid size at day 7 with treated 1, 5,10 and 20 µM Chrysotoxine, respectively.
体内研究
(In Vivo)

Chrysotoxine (25 mg/kg,静脉注射;100 mg/kg,口服;一次) 在 Sprague-Dawley 大鼠模型中快速排泄并且有低生物利用度的特点[2] Pharmacokinetic parameters of Chrysotoxine in Sprague-Dawley rats[2]

Parameters Intravenous Oral
AUC0–t (μg h/L) 1257.6 ± 570.7 172.8 ± 118.9
AUC0–∞ (μg h/L) 1270.1 ± 560.6 202.5 ± 123.8
MRT0–t (μg h/L) 0.467 ± 0.056 1.2 ± 0.46
MRT0–∞ (μg h/L) 0.59 ± 0.21 2.4 ± 1.8
t1/2Z ( h) 1.4 ± 0.76 1.7 ± 1.1
Tmax ( h) / 0.098 ± 0.040
CLZ /F (L/h/kg) 22.9 ± 11.2 668.7 ± 396.9
VZ /F (L/kg) 55.3 ± 54.1 1443.2 ± 943.0
Cmax (μg/L) 4961.2 ± 3254.8 408.8 ± 160.5
F (%) / 3.4 ± 2.4

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

318.36

Formula

C18H22O5

CAS 号
性状

固体

颜色

White to off-white

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 6.37 mg/mL (20.01 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1411 mL 15.7055 mL 31.4110 mL
5 mM 0.6282 mL 3.1411 mL 6.2822 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

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动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

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动物的平均体重

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每只动物的给药体积

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动物数量

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计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1411 mL 15.7055 mL 31.4110 mL 78.5275 mL
5 mM 0.6282 mL 3.1411 mL 6.2822 mL 15.7055 mL
10 mM 0.3141 mL 1.5705 mL 3.1411 mL 7.8527 mL
15 mM 0.2094 mL 1.0470 mL 2.0941 mL 5.2352 mL
20 mM 0.1571 mL 0.7853 mL 1.5705 mL 3.9264 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Chrysotoxine
目录号:
HY-123298
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