| Identification | Back Directory | [Name]
SU14813 | [CAS]
627908-92-3 | [Synonyms]
SU14813
CS-1149
SU-14813; SU 14813
SU14813(Random Configuration)
5-[(Z)-(5-Fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N- [ 2-hydroxy-3-(4-morpholinyl)propyl]-2,4-dimethyl-1H-pyrrole-3-carb
5-[(5-Fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-(4-morpholinyl)propyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
1H-Pyrrole-3-carboxamide, 5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-(4-morpholinyl)propyl]-2,4-dimethyl- | [Molecular Formula]
C23H27FN4O4 | [MOL File]
627908-92-3.mol | [Molecular Weight]
442.48 |
| Chemical Properties | Back Directory | [Boiling point ]
685.6±55.0 °C(Predicted) | [density ]
1.341 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 44 mg/mL (99.44 mM; Need ultrasonic) | [form ]
Powder | [pka]
11.24±0.20(Predicted) |
| Hazard Information | Back Directory | [Biological Activity]
SU14813 (SU 014813) is a multi-receptor tyrosine kinase inhibitor with IC50 values of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit), respectively. It has potent antiangiogenic and antitumor activities. | [in vitro]
SU14813 inhibits ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets. It inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells) , PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR- 2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC 50 values of 5.2, 9.9, and 11.2 nM, respectively. Also it inhibits the growth of U-118MG with an IC 50 of 50 to 100 nM. | [in vivo]
SU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduces growth of various established xenografts derived from human or rat tumor cell lines. Treatment in combination with docetaxel significantly enhances both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone. | [target]
| Target | Value | VEGFR1
(Cell-free assay) | 2 nM | PDGFRβ
(Cell-free assay) | 4 nM | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> KIT
(Cell-free assay) 15 nM | VEGFR2
(Cell-free assay) | 50 nM |
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