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

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.

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Chrysotoxine Chemical Structure

Chrysotoxine Chemical Structure

CAS No. : 156951-82-5

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Based on 1 publication(s) in Google Scholar

Chrysotoxine Related Antibodies

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Description

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].

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]
In Vitro

Chrysotoxine (50 nM, 24 h) reduces cell viability and increases apoptosis level in H460 and H23 cells[1].
Chrysotoxine (5-20 nM, 72 h) suppresses the CSC populations in H460 and H23 cells[1].
Chrysotoxine (0-20 nM, overnight) decreases the stemness of H460 and H23 cells by suppressing the Src-Akt activating mechanism[1].

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

Chrysotoxine Related Antibodies

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.
In Vivo

Chrysotoxine (25 mg/kg for i.v; 100 mg/kg for p.o;once) rapidly excreted and has low bioavailability in Sprague-Dawley rats model[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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

318.36

Formula

C18H22O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=C(C=C(C=C1OC)CCC2=CC=C(C(OC)=C2)OC)OC
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.37 mg/mL (20.01 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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Chrysotoxine Related Classifications

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.

Keywords:

Chrysotoxine156951-82-5SrcAktApoptosisPKBProtein kinase BH460H23Cancer stem cellsCSCsLung cancerSprague-Dawley ratsInhibitorinhibitorinhibit

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