Description
| Description | PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM). |
| Targets&IC50 | PYK2:11 nM, FAK:2 nM |
| Kinase Assay | In Vitro Kinase Assays and Selectivity Screening : To measure Mps1 activity, 25 ng of recombinant, full-length enzyme is incubated in reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.01% Triton X-100 and 5 μM Myelin basic protein (MBP)) containing vehicle (DMSO alone) or inhibitors. Forty μM ATP (2xKm) is added with 1 μCi [γ-33P]ATP and the reaction is incubated at room temperature for 45 minutes. Reactions are terminated with 3% phosphoric acid and transferred to P81 filter plates. Samples are washed in 1% phosphoric acid and 33P radioactivity is measured on a TopCount scintillation reader. In-house kinase assays are all carried out at 2xKm ATP concentrations. MPI-0479605 (500 nM) is also screened against a larger kinase panel. |
| Molecular Weight |
506.5 |
| Formula | C22H21F3N6O3S |
| CAS No. | 717906-29-1 |
Storage
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Solubility Information
DMSO: 25.3 mg/mL (50 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
