VPC03090
VPC03090 is an orally active prodrug of S1P1/3 antagonist. VPC03090 is phosphorylated by sphingosine kinase 2 (SK2) to form its active form VPC03090-P. VPC03090 reduces tumor volume in mouse breast cancer models. VPC03090 can be used in research related to breast cancer.
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- CAS. Nr.: 1392202-91-3
- Formel: C19H31NO
- Molecular Weight:289.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
VPC03090 (10 mg/kg; p.o.; single administration) is rapidly phosphorylated to VPC03090-P in C57BL/6J mice[1].
VPC03090 (30 mg/kg; i.p.; single administration) results in undetectable plasma levels of VPC03090-P in sphingosine kinase 2 gene knockout mice, which confirms that sphingosine kinase 2 is essential for the phosphorylation of VPC03090 in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6 weeks of age, orthotopic syngeneic model via injection of 1×105 4T1 mammary cancer cells into the fourth mammary gland fat pad)[1]
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Dosage:6.2 mg/kg/day
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Administration:i.p.; daily; 14 days
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Result:Reduced median tumor volume approximately 3-fold compared with vehicle-treated controls.
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Animal Model:C57BL/6j[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Appeared in plasma as phosphorylated active form VPC03090-P within 30 minutes post-dose.
Maintained an approximate 1:1 ratio of phosphorylated (VPC03090-P) to alcohol (VPC03090) species for 6 days post-dose.
Had a VPC03090-P half-life of 30 hours.
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Animal Model:Sphingosine kinase 2 null (hybrid C57BL/6 and SV129 genetic background)[1]
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Dosage:30 mg/kg
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Administration:i.p.; single dose
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Result:Resulted in micromolar-range plasma VPC03090 concentrations, but VPC03090-P was undetectable (below the LC-MS limit of detection of ~2.5 nM).
Chemical Information
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CAS. Nr. 1392202-91-3
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Molecular Weight 289.46
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Formel C19H31NO
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SMILES
OCC1(CC(C1)C2=CC=CC(CCCCCCCC)=C2)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Kennedy PC, et al. Characterization of a sphingosine 1-phosphate receptor antagonist prodrug. The Journal of pharmacology and experimental therapeutics. 2011 Sep;338(3):879-89. [Content Brief]
[2]. Kornienko A, et al. Toward a Cancer Drug of Fungal Origin. Medicinal research reviews. 2015 Sep;35(5):937-67. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
VPC03090 Related Classifications
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