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].

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
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 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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