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- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
Biological Activity
CP-690550 (Tofacitinib citrate) is an orally available, highly selective inhibitor of the Janus kinase (JAK) family of enzymes.
Targets
| Target | Value |
|---|---|
| JAK3 | IC50: 1nM |
| JAK2 | IC50: 20nM |
| JAK1 | IC50: 112nM |
| ROCK2 | IC50: 3.4μM |
| LCK | IC50: 3.87μM |
| IRK | IC50: >10μM |
| CDK2 | IC50: >10μM |
| CDK5 | IC50: >10μM |
| EGFR | IC50: >10μM |
| MAPK2/ERK2 | IC50: >10μM |
| JNK1/SAPK1c | IC50: >10μM |
| SAPK2a/p38 | IC50: >10μM |
| SAPK2b/p38b2 | IC50: >10μM |
| SAPK3/p38g | IC50: >10μM |
| SAPK4/p38d | IC50: >10μM |
| MAPKAPK2 | IC50: >10μM |
| MAPKAP-K1b | IC50: >10μM |
| MSK1 | IC50: >10μM |
| PRAK | IC50: >10μM |
| PKA | IC50: >10μM |
| PKCα | IC50: >10μM |
| PDK-1 | IC50: >10μM |
| PKBα | IC50: >10μM |
| SGK | IC50: >10μM |
| p70S6K | IC50: >10μM |
| GSK-3β | IC50: >10μM |
| AMPK | IC50: >10μM |
| Chk1 | IC50: >10μM |
| CK2 | IC50: >10μM |
| PHK | IC50: >10μM |
| CSK | IC50: >10μM |
| CDK2/CyclinA | IC50: >10μM |
| PI3K | IC50: >10μM |
| In vitro (25°C) | DMSO | Warmed: 94 mg/mL (186.32 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 0.5% methylcellulose | 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 | 19.82 mL | 99.11 mL | 198.22 mL |
| 0.5 mM | 3.96 mL | 19.82 mL | 39.64 mL |
| 1 mM | 1.98 mL | 9.91 mL | 19.82 mL |
| 5 mM | 0.4 mL | 1.98 mL | 3.96 mL |
*The above data is based on the productmolecular weight 504.5 . 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 | A10241 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 540737-29-9 |
| Formula | C16H20N6O.C6H8O7 |
| M. Wt | 504.5 |
| Purity | >98% |
| Synonyms | CP690550, tasocitinib citrate, CP-690,550 |
| SMILES | C[[email protected]@H]1CCN(C[[email protected]@H]1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N.C(C(=O)O)C(CC(=O)O)(C(=O)O)O |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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