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Biological Activity
PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.
Targets
| Target | Value |
|---|---|
| FAK | IC50: 1.5nM |
| PYK2 | IC50: 13nM |
| CDK2/CyclinE | IC50: 30nM |
| CDK3/CyclinE | IC50: 47nM |
| CDK1/CyclinB | IC50: 58nM |
| CDK7/CyclinH/MAT1 | IC50: 97nM |
| FLT3 | IC50: 97nM |
| GSK-3α | IC50: 101nM |
| CDK5/p35 | IC50: 120nM |
| GSK-3β | IC50: 133nM |
| AuroraA | IC50: 145nM |
| CDK2/CyclinA | IC50: 227nM |
| YES | IC50: 294nM |
| MAPK1 | IC50: 340nM |
| Fyn | IC50: 377nM |
| LCK | IC50: 408nM |
| IGF-1R | IC50: >500nM |
| PKA | IC50: 620nM |
| c-Src | IC50: 797nM |
| CDK4 | IC50: >1μM |
| CDK6/CyclinD2 | IC50: >1μM |
| Chk1 | IC50: >1μM |
| Chk2 | IC50: >1μM |
| EGFR | IC50: >1μM |
| EphB2 | IC50: >1μM |
| FGFR3 | IC50: >1μM |
| Abl | IC50: >1μM |
| Fms | IC50: >1μM |
| IKKα | IC50: >1μM |
| IKKβ | IC50: >1μM |
| JNK1α1 | IC50: >1μM |
| MEK1 | IC50: >1μM |
| p70S6K | IC50: >1μM |
| PKBα | IC50: >1μM |
| PKBβ | IC50: >1μM |
| PKBγ | IC50: >1μM |
| PKCα | IC50: >1μM |
| PKCβ2 | IC50: >1μM |
| PKCδ | IC50: >1μM |
| TrkB | IC50: >2.5μM |
| PDGFRβ | IC50: >3μM |
| In vitro (25°C) | DMSO | Warmed: 14 mg/mL (21.03 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 4% DMSO+30% PEG 300+ddH2O | 2 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 | 15.02 mL | 75.11 mL | 150.23 mL |
| 0.5 mM | 3 mL | 15.02 mL | 30.05 mL |
| 1 mM | 1.5 mL | 7.51 mL | 15.02 mL |
| 5 mM | 0.3 mL | 1.5 mL | 3 mL |
*The above data is based on the productmolecular weight 665.66. 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 | A12580 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 939791-38-5 |
| Formula | C21H20F3N7O3S.C6H6O3S |
| M. Wt | 665.66 |
| Purity | >98% |
| Synonyms | PF00562271, PF 00562271 |
| SMILES | CN(C1=C(C=CC=N1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)C4)S(=O)(=O)C.C1=CC=C(C=C1)S(=O)(=O)O |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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