N-Desethyl Sunitinib - CAS 356068-97-8
Catalog number: 356068-97-8
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
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.
SU11662; SU 11662; SU-11662
Canonical SMILES:
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related PDGFR Products

CAS 1123491-15-5 DMPQ dihydrochloride

DMPQ dihydrochloride
(CAS: 1123491-15-5)

DMPQ dihydrochloride is a potent and selective inhibitor of human vascular β-type platelet derived growth factor receptor tyrosine kinase (PDGFRβ) (IC50 = 80 nM...

CAS 670220-88-9 Crenolanib

(CAS: 670220-88-9)

Crenolanib is an orally bioavailable small molecule, targeting the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Cren...

CAS 796967-16-3 Linifanib

(CAS: 796967-16-3)

Description of Linifanib: Linifanib is an orally bioavailable, small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. L...

CAS 1351522-04-7 AC710

(CAS: 1351522-04-7)

AC710 is a potent, selective platelet-derived growth factor receptor-family kinase inhibitor with potential anticancer activity. AC710 is now a preclinical deve...

CAS 5812-07-7 SU 4312

SU 4312
(CAS: 5812-07-7)

SU 4312 is a potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases (IC50 = 0.8 and 19.4 μM, respectively) wirth selectivity over EGFR and c-Src tyr...

CAS 926037-48-1 Radotinib

(CAS: 926037-48-1)

Radotinib, also known as IY-5511, is an orally available, hydrochloride salt form of radotinib, a second-generation tyrosine kinase inhibitor of Bcr-Abl fusion ...

CAS 343787-29-1 CP-673451

(CAS: 343787-29-1)

CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and a...

CAS 251356-45-3 SU 16f

SU 16f
(CAS: 251356-45-3)

SU 16f is a potent and selective platelet-derived growth factor receptor β (PDGFRβ) inhibitor (IC50 = 10 nM), displaying > 14-fold, > 229-fold and > 10000-fold ...

CAS 635702-64-6 Pazopanib HCl

Pazopanib HCl
(CAS: 635702-64-6)

Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 1...

CAS 877874-85-6 KG 5

KG 5
(CAS: 877874-85-6)

KG 5 is a B-Raf allosteric and PDGFRβ inhibitor. It inhibits FLT3, KIT and c-Raf. It arrests cells in prometaphase and inhibits growth of renal and pancreatic t...

CAS 883986-34-3 AZD2932

(CAS: 883986-34-3)

AZD2932 is a new quinazoline ether inhibitor and is a high affinity inhibitor of VEFGR-2 and PDGFR. It has a balanced ~1:1 ratio of activity vs both VEGFR-2 an...

CAS 444731-52-6 Pazopanib

(CAS: 444731-52-6)

Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 1...

CAS 849643-15-8 SU14813 maleate

SU14813 maleate
(CAS: 849643-15-8)

SU14813 maleate is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growt...

CAS 1351522-05-8 AC710 Mesylate

AC710 Mesylate
(CAS: 1351522-05-8)

AC710 Mesylate is a potent, selective PDGFR-family kinases inhibitor with Kd values of 0.6 nM/1.0 nM/1.3 nM/1.0 nM for FLT3/KIT/PDGFRα/PDGFRβ respect...

CAS 874819-74-6 Toceranib phosphate

Toceranib phosphate
(CAS: 874819-74-6)

Toceranib phosphate is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor...

CAS 341031-54-7 Sunitinib Malate

Sunitinib Malate
(CAS: 341031-54-7)

Sunitinib (marketed as Sutent by Pfizer, and previously known as SU11248) is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor th...

CAS 356068-94-5 Toceranib

(CAS: 356068-94-5)

Toceranib (CAS 356068-94-5) is a potent ATP-competitive PDGFR and VEGFR inhibitor (Ki = 5 and 6 nM, respectively); inhibits phosphorylation of c-Kit and suppres...

CAS 1005780-62-0 TAK-593

(CAS: 1005780-62-0)

TAK-593 is an oral formulation containing a small-molecule receptor tyrosine kinase inhibitor of both vascular endothelial growth factor receptor (VEGFR) and pl...

CAS 252916-29-3 Orantinib

(CAS: 252916-29-3)

TSU-68 (SU6668; Orantinib) is a novel multiple receptor tyrosine kinase inhibitor with IC50 of 2.1 μM, 8 nM and 1.2 μM for VEGF-R1, PDGF-Rβ and FGF-R1, respecti...

CAS 326914-10-7 SU11652

(CAS: 326914-10-7)

SU11652 is a cell-permeable and sunitinib-like inhibitor of tyrosine kinase receptor (RTK) and angiogenesis with antineoplastic property. It selectively inhibit...

Chemical Structure

CAS 356068-97-8 N-Desethyl Sunitinib

Quick Inquiry

Verification code

Featured Items