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N-Desethyl Sunitinib

Cat. No. M5066
N-Desethyl Sunitinib Structure
Synonym:

SU11662

Size Price Availability
10mM*1mL USD 350  USD350 Out of stock
5mg USD 240  USD240 Out of stock
10mg USD 360  USD360 Out of stock
50mg USD 960  USD960 Out of stock
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Quality Control & Documentation
Biological Activity

N-Desethyl Sunitinib is a major and pharmacologically active metabolite of the tyrosine kinase inhibitor and anticancer compound Sunitinib. Sunitinib also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Sunitinib exhibits antiangiogenic and antitumor activity in multiple xenograft models.

Chemical Information
Molecular Weight 370.42
Formula C20H23FN4O2
CAS Number 356068-97-8
Form Solid
Solubility (25°C) 10 mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Elena Marangon, et al. A new high-performance liquid chromatography-tandem mass spectrometry method for the determination of sunitinib and N-desethyl sunitinib in human plasma: Light-induced isomerism overtaking towards therapeutic drug monitoring in clinical routine

[2] Xiao Chen, et al. Determination of sunitinib and its active metabolite, N-desethyl sunitinib in mouse plasma and tissues by UPLC-MS/MS: assay development and application to pharmacokinetic and tissue distribution studies

[3] Nienke A G Lankheet, et al. Quantification of sunitinib and N-desethyl sunitinib in human EDTA plasma by liquid chromatography coupled with electrospray ionization tandem mass spectrometry: validation and application in routine therapeutic drug monitoring

[4] Rana Rais, et al. Quantitation of unbound sunitinib and its metabolite N-desethyl sunitinib (SU12662) in human plasma by equilibrium dialysis and liquid chromatography-tandem mass spectrometry: application to a pharmacokinetic study

[5] Seng Chuan Tang, et al. P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) restrict brain accumulation of the active sunitinib metabolite N-desethyl sunitinib

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Keywords: N-Desethyl Sunitinib, SU11662 supplier, Metabolite/Endogenous Metabolite, inhibitors, activators


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