326914-17-4
Chemical Structure
SU11657
Synonym(s): N,N-Dimethyl sunitinib
- CAS No.: 326914-17-4
- Formula:C20H23FN4O2
- Molecular Weight:370.43
IUPAC Name: (Z)-N-(2-(dimethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide
InChIKey: MBTDIENWIYANIG-GDNBJRDFSA-N
SMILES: C(=C\1/C=2C(NC1=O)=CC=C(F)C2)\C3=C(C)C(C(NCCN(C)C)=O)=C(C)N3
Biological Activity: SU11657 (N,N-Dimethyl sunitinib) is an orally active multi-targeted tyrosine kinase inhibitor with IC50 values of 0.04 μM (c-Kit), 0.005 μM (PDGFR), 0.013 μM (VEGFR1), 0.017 μM (VEGFR2) and 50 nM (FLT3), respectively. SU11657 exhibits anti-angiogenic activity. SU11657 delays leukemia progression, synergizes with ATRA (HY-14649) to reduce leukemia burden, and inhibits symptoms and tissue damage associated with rheumatoid arthritis. SU11657 can be used in research related to FLT3-mutated acute promyelocytic leukemia, rheumatoid arthritis, neuroblastoma, and benign/atypical meningioma[1][2][3][4].
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SU11657 | SU11657 (N,N-Dimethyl sunitinib) is an orally active multi-targeted tyrosine kinase inhibitor with IC50 values of 0.04 μM (c-Kit), 0.005 μM (PDGFR), 0.013 μM (VEGFR1), 0.017 μM (VEGFR2) and 50 nM (FLT3), respectively. SU11657 exhibits anti-angiogenic activity. SU11657 delays leukemia progression, synergizes with ATRA (HY-14649) to reduce leukemia burden, and inhibits symptoms and tissue damage associated with rheumatoid arthritis. SU11657 can be used in research related to FLT3-mutated acute promyelocytic leukemia, rheumatoid arthritis, neuroblastoma, and benign/atypical meningioma. | |||||||||||||||||||||
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- [1]. Sohal J, et al. A model of APL with FLT3 mutation is responsive to retinoic acid and a receptor tyrosine kinase inhibitor, SU11657. Blood. 2003 Apr 15;101(8):3188-97. [Content Brief]
- [2]. De Bandt M, et al. Blockade of vascular endothelial growth factor receptor I (VEGF-RI), but not VEGF-RII, suppresses joint destruction in the K/BxN model of rheumatoid arthritis. Journal of immunology (Baltimore, Md. : 1950). 2003 Nov 01;171(9):4853-9. [Content Brief]
- [3]. Bäckman U, et al. The selective class III/V receptor tyrosine kinase inhibitor SU11657 inhibits tumor growth and angiogenesis in experimental neuroblastomas grown in mice. Pediatric research. 2005 May;57(5 Pt 1):690-5. [Content Brief]
- [4]. Milker-Zabel S, et al. SU11657 enhances radiosensitivity of human meningioma cells. International journal of radiation oncology, biology, physics. 2008 Mar 15;70(4):1213-8. [Content Brief]
Keywords
