N-Desethyl Sunitinib - CAS 356068-97-8
Catalog number: 356068-97-8
Category: Inhibitor
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Molecular Formula:
C20H23FN4O2
Molecular Weight:
370.42
COA:
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Targets:
PDGFR
Description:
N-Desethyl Sunitinib is a major and pharmacologically active metabolite of the tyrosine kinase inhibitor and anticancer drug Sunitinib. Sunitinib also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Sunitinib exhibits antiangiogenic and antitumor activity in multiple xenograft models.
Purity:
>98%
Synonyms:
SU11662; SU 11662; SU-11662
MSDS:
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InChIKey:
LIZNIAKSBJKPQC-GDNBJRDFSA-N
InChI:
InChI=1S/C20H23FN4O2/c1-4-22-7-8-23-20(27)18-11(2)17(24-12(18)3)10-15-14-9-13(21)5-6-16(14)25-19(15)26/h5-6,9-10,22,24H,4,7-8H2,1-3H3,(H,23,27)(H,25,26)/b15-10-
Canonical SMILES:
CCNCCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C
1.Quantitation of sunitinib, an oral multitarget tyrosine kinase inhibitor, and its metabolite in urine samples by nonaqueous capillary electrophoresis time of flight mass spectrometry.
Rodríguez J1, Castañeda G1, Muñoz L1, Villa JC2. Electrophoresis. 2015 Jul;36(14):1580-7. doi: 10.1002/elps.201400588. Epub 2015 May 20.
A rapid, sensitive, and specific method was developed and validated using a nonaqueous-capillary electrophoresis method with TOF-MS for determination of sunitinib and N-desethyl sunitinib in human urine. In order to avoid ionic suppression a urine samples dilution with methanol 1:10 previous step was used. This was the only treatment step to urine samples before the injection. Despite this dilution of the urine, the detection limit was as low as 0.07 mg/L for sunitinib and 0.15 mg/L for N-desethyl sunitinib. Separation of compounds was achieved with a mixture of 5 mM ammonium formate in methanol. The calibration curves were linear over the range of 0.5-50.0 mg/L for the two analyzed compounds. The within-run and between-run precisions were within 5%, while the accuracy ranged from 96.0 to 100.4%. This method can be used in routine clinical practice to monitor sunitinib and N-desethyl sunitinib drugs in the urine of cancer patients treated with once daily administration.
2.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.
Chen X1, Wang Z, Liu M, Liao M, Wang X, Du H, Chen J, Yao M, Li Q. Biomed Chromatogr. 2015 May;29(5):679-88. doi: 10.1002/bmc.3331. Epub 2014 Oct 8.
A simple, sensitive and specific method using ultraperformance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) was developed to determine sunitinib and N-desethyl sunitinib in mouse plasma and tissues. The analytes were separated by an isocratic mobile phase consisting of acetonitrile and buffer solution (water with 0.1% formic acid and 5 m m ammonium acetate; 40: 60, v/v) running at a flow rate of 0.35 mL/min for 2 min. Quantification was performed using a mass spectrometer by multiple reaction monitoring in positive electrospray ionization mode. The transition was monitored at m/z 399 → 283, m/z 371 → 283 and m/z 327 → 270 for sunitinib, N-desethyl sunitinib and internal standard, respectively. Calibration curves were linear over concentration ranges of 2-500, 0.5-50 and 1-250 ng/mL for plasma, heart and other biosamples. The method was successfully applied to animal experiments. The pharmacokinetic study indicated that sunitinib was eliminated quickly in mice with a half-life of 1.
3.Integrated semi-physiological pharmacokinetic model for both sunitinib and its active metabolite SU12662.
Yu H1, Steeghs N, Kloth JS, de Wit D, van Hasselt JG, van Erp NP, Beijnen JH, Schellens JH, Mathijssen RH, Huitema AD. Br J Clin Pharmacol. 2015 May;79(5):809-19. doi: 10.1111/bcp.12550.
AIMS: Previously published pharmacokinetic (PK) models for sunitinib and its active metabolite SU12662 were based on a limited dataset or lacked important elements such as correlations between sunitinib and its metabolite. The current study aimed to develop an improved PK model that circumvented these limitations and to prove the utility of the PK model in treatment optimization in clinical practice.
4.Role of the lean body mass and of pharmacogenetic variants on the pharmacokinetics and pharmacodynamics of sunitinib in cancer patients.
Narjoz C1, Cessot A, Thomas-Schoemann A, Golmard JL, Huillard O, Boudou-Rouquette P, Behouche A, Taieb F, Durand JP, Dauphin A, Coriat R, Vidal M, Tod M, Alexandre J, Loriot MA, Goldwasser F, Blanchet B. Invest New Drugs. 2015 Feb;33(1):257-68. doi: 10.1007/s10637-014-0178-2. Epub 2014 Oct 25.
INTRODUCTION: Sunitinib is a multikinase inhibitor active in various cancers types including renal cancers and endocrine tumors. The study analyzed the influence of the lean body mass (LBM) and of pharmacogenetic variants on the exposure to sunitinib and its active metabolite, SU12662, and on sunitinib toxicity and clinical activity.
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CAS 356068-97-8 N-Desethyl Sunitinib

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