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- Aaron Y. Lai, .et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
Biological Activity
Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
Targets
| PDGFRβ (Cell-free assay) | FGFR1 (Cell-free assay) | Flk1 (Cell-free assay) | ||
| 8 nM(Ki) | 1.2 μM(Ki) | 2.1 μM(Ki) |
| In vitro (25°C) | DMSO | 55 mg/mL (177.22 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 32.22 mL | 161.08 mL | 322.16 mL |
| 0.5 mM | 6.44 mL | 32.22 mL | 64.43 mL |
| 1 mM | 3.22 mL | 16.11 mL | 32.22 mL |
| 5 mM | 0.64 mL | 3.22 mL | 6.44 mL |
*The above data is based on the productmolecular weight 310.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10953 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 252916-29-3 |
| Formula | C18H18N2O3 |
| M. Wt | 310.4 |
| Purity | >98% |
| Synonyms | TSU68 |
| SMILES | CC1=C(NC(=C1CCC(=O)O)C)/C=C\2/C3=CC=CC=C3NC2=O |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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