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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $50 | In Stock | |
10 mg | $74 | In Stock | |
25 mg | $148 | In Stock | |
50 mg | $261 | In Stock | |
100 mg | $447 | In Stock | |
200 mg | $659 | In Stock | |
1 mL x 10 mM (in DMSO) | $59 | In Stock |
Description | PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM). |
Targets&IC50 | PYK2:11 nM, FAK:2 nM |
In vitro | PF-431396 consistently inhibits protein tyrosine kinase phosphorylation under both calcium deficiency and the presence of Ca/W-7. It also blocks tyrosine phosphorylation of Pyk2 and FAK induced by anti-Ig- and aggregated LFA-1 in A20 cells, thereby inhibiting B cell proliferation. |
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 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 25.3 mg/mL (50 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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