356068-97-8
356068-97-8
Chemical Structure
N-Desethyl Sunitinib
Synonym(s): SU-12662
- CAS No.: 356068-97-8
- Formula:C20H23FN4O2
- Molecular Weight:370.42
IUPAC Name: (Z)-N-(2-(ethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide
InChIKey: LIZNIAKSBJKPQC-GDNBJRDFSA-N
SMILES: O=C1NC2=CC=C(F)C=C2/C1=C/C3=C(C)C(C(NCCNCC)=O)=C(C)N3
Biological Activity: N-Desethyl Sunitinib (SU-12662) is a metabolite of Sunitinib (HY-10255A). N-Desethyl Sunitinib serves as a good transport substrate for human ABCB1, ABCG2 and murine ABCG2[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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N-Desethyl Sunitinib | 99.81% | N-Desethyl Sunitinib (SU-12662) is a metabolite of Sunitinib (HY-10255A). N-Desethyl Sunitinib serves as a good transport substrate for human ABCB1, ABCG2 and murine ABCG2. | ||||||||||||||||||||
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N-Desethyl Sunitinib (Standard) | ≥98% | N-Desethyl Sunitinib (Standard) is the analytical standard of N-Desethyl Sunitinib. This product is intended for research and analytical applications. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively. | ||||||||||||||||||||
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N-Desethyl Sunitinib-d4 TFA | N-Desethyl Sunitinib-d4 (SU-12662-d4) TFA is deuterium-labeled N-Desethyl Sunitinib (HY-10873). | |||||||||||||||||||||
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N-Desethyl Sunitinib-d5 | 99.9% | N-Desethyl Sunitinib-d5 is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively. | ||||||||||||||||||||
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N-Desethyl Sunitinib-d5 hydrochloride | N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively. | |||||||||||||||||||||
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References
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[1]. Li Sun, et al. Discovery of 5-[5-Fluoro-2-oxo-1,2-dihydroindol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic Acid (2-Diethylaminoethyl)amide, a Novel
Tyrosine Kinase Inhibitor Targeting Vascular Endothelial and
Platelet-Derived Growth Factor Receptor Tyrosine Kinase. J. Med. Chem. 2003, 46, 1116-1119 - [2]. Tang SC, et al. P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) restrict brain accumulation of the active sunitinib metabolite N-desethyl sunitinib. J Pharmacol Exp Ther. 2012;341(1):164-173. [Content Brief]
- [3]. Li JY,et al. Preclinical PK/PD model for combined administration of erlotinib and sunitinib in the treatment of A549 human NSCLC xenograft mice. Acta Pharmacol Sin. 2016 Jul;37(7):930-40. [Content Brief]
