627908-92-3
SU14813
CAS: 627908-92-3
Molecular Formula: C23H27FN4O4
627908-92-3 - Names and Identifiers
627908-92-3 - Physico-chemical Properties
| Molecular Formula | C23H27FN4O4 |
| Molar Mass | 442.48 |
| Density | 1.341 |
| Boling Point | 685.6±55.0 °C(Predicted) |
| Solubility | DMSO: 44 mg/mL (99.44 mM), Need ultrasonic( < 1 mg/ml refers to the product slightly soluble or insoluble) |
| pKa | 11.24±0.20(Predicted) |
| Storage Condition | -20℃ |
| Use | SU14813 is a multi-target receptor tyrosine kinase inhibitor. The IC50 values of VEGFR2,VEGFR1,PDGFRβ and KIT are 50,2,4 and 15 nM respectively. Related CAS#452105-23-6 ( SU14813 double Z isomer)627908-92-3 (SU1481free base);849643-15-8 (SU1481 maleate) |
| Target | VEGFR1; VEGFR2; PDGFRβ; KIT; VEGFR Kinases; Tyrosine |
| In vitro study | SU14813 inhibits ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets. SU14813 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. SU14813 inhibits the growth of U-118MG with an IC 50 of 50 to 100 nM. |
| In vivo study | 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. |
627908-92-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.26 ml | 11.3 ml | 22.599 ml |
| 5 mM | 0.452 ml | 2.26 ml | 4.52 ml |
| 10 mM | 0.226 ml | 1.13 ml | 2.26 ml |
| 5 mM | 0.045 ml | 0.226 ml | 0.452 ml |
Last Update：2024-01-02 23:10:35
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