1. Apoptosis
    Protein Tyrosine Kinase/RTK
    Metabolic Enzyme/Protease
    Anti-infection
  2. Apoptosis
    VEGFR
    Lipoxygenase
    Bacterial
  3. Xanthatin

Xanthatin 

Cat. No.: HY-N3032 Purity: 99.79%
Handling Instructions

Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer.

For research use only. We do not sell to patients.

Xanthatin Chemical Structure

Xanthatin Chemical Structure

CAS No. : 26791-73-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 135 In-stock
Estimated Time of Arrival: December 31
5 mg USD 125 In-stock
Estimated Time of Arrival: December 31
10 mg USD 215 In-stock
Estimated Time of Arrival: December 31
50 mg USD 775 In-stock
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100 mg USD 1335 In-stock
Estimated Time of Arrival: December 31
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Description

Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity[1]. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer[2].

IC50 & Target

IC50: apoptosis; 3.8 μM (VEGFR2 kinase); 2.63 µg/mL (T. b. brucei)[1]

In Vitro

Xanthatin is against T. b. brucei with an IC50 value of 2.63 µg/mL and exhibits weak irreversible inhibition of parasite specific trypanothione reductase[1].
Xanthatin (0-40 μM; 24 hours) has obscure inhibition effect on the proliferation of HUVEC in the absence of VEGF[2].
Xanthatin (5-40 μM; 24 hours) inhibits breast cancer cell proliferation in a dose responsive manner. Xanthatin inhibits HCC1937, MDA-MB-415, SK-BR-3, MCF-7 and MDA-MB-231 with IC50 values of 81 μM, 31 μM, 38 μM, 30 μM, and 17 μM, respectively[2].
Xanthatin (0-10 μM; 24 hours) dose dependently suppresses the phosphorylation of STAT3 (Ser727), at the same time, it also results in a rapid dephosphorylation of down-stream kinases of STAT3, including PI3K and Akt, including PI3K (p-PI3K p85 tyr458) and Akt[2].

Cell Proliferation Assay[2]

Cell Line: HUVEC cells
Concentration: 0 μM, 5 μM, 10 μM, 15 μM, 20 μM, 30 μM, 40 μM
Incubation Time: 24 hours
Result: Inhibited cell growth from dose 10 μM in the presence of vEGF.

Cell Viability Assay[2]

Cell Line: HCC1937, MDA-MB-415, SK-BR-3, MCF-7 and MDA-MB-231 cells
Concentration: 5, 10, 15, 20, 30, and 40 μM
Incubation Time: 24 hours
Result: Inhibited breast cancer cell growth.

Western Blot Analysis[2]

Cell Line: HUVEC cells
Concentration: 0, 3, and 10 μM
Incubation Time: 24 hours
Result: Inhibited VEGFR2 downstream signaling pathways and blocked VEGF-induced STAT3 activation in HUVEC.
In Vivo

Xanthatin (intragastric administration; 20 mg/kg; once daily; 25 days) leads to significant inhibition of tumor volume. And this compound is well-tolerated and exhibits no significant difference in weight compares to the vehicle group[2].

Animal Model: Transplanted MDA-MB-231 cells into mice and constucted human breast cancer xenograft mouse model[2] 
Dosage: 20 mg/kg; once daily; 25 days
Administration: Intragastric administration
Result: Supressed tumor growth and tumor angiogenesis in vivo.
Molecular Weight

246.30

Formula

C₁₅H₁₈O₃

CAS No.

26791-73-1

SMILES

C=C1[[email protected]]2([H])[[email protected]@](C[[email protected]](C)C(/C=C/C(C)=O)=CC2)([H])OC1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (1015.02 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0601 mL 20.3004 mL 40.6009 mL
5 mM 0.8120 mL 4.0601 mL 8.1202 mL
10 mM 0.4060 mL 2.0300 mL 4.0601 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.44 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.44 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.44 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

XanthatinApoptosisVEGFRLipoxygenaseBacterialVascular endothelial growth factor receptorLOXT. b. bruceiantiinflammatoryparasiteapoptosis5-lipoxygenasebreastcancerInhibitorinhibitorinhibit

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