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PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.
Targets
| Aurora A | Aurora B | FLT1 | FAK | TrkA |
| 0.8 nM | 5 nM | 10 nM | 22 nM | 30 nM |
| In vitro (25°C) | DMSO | 0.4 mg/mL (<1 mM) | |
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 2% Cremophor EL, 2% N,N-dimethylacetamide, pH 5.0 | 30 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. |
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| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 21.08 mL | 105.38 mL | 210.76 mL |
| 0.5 mM | 4.22 mL | 21.08 mL | 42.15 mL |
| 1 mM | 2.11 mL | 10.54 mL | 21.08 mL |
| 5 mM | 0.42 mL | 2.11 mL | 4.22 mL |
*The above data is based on the productmolecular weight 474.48. 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.
Chemical Properties
| Catalog Num | A11171 |
|---|---|
| Actions | Inhibitor |
| M. Wt | 474.48 |
| Formula | C23H25F3N6O2 |
| Solubility | DMSO |
| Purity | >98% |
| Storage | at -20°C 3 years Powder |
| CAS No. | 942487-16-3 |
| Synonyms | PF03814735 |
| SMILES | CC(=O)NCC(=O)N1[[email protected]]2CC[[email protected]@H]1C3=C2C=CC(=C3)NC4=NC=C(C(=N4)NC5CCC5)C(F)(F)F |
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