生物活性
Baricitinib，也称为INCB028050或LY3009104，是一种选择性口服可生物利用的JAK1/JAK2抑制剂，对JAK1（5.9 nM）和JAK2（5.7 nM）具有纳摩尔浓度。
Targets
| Target | Value |
| JAK2 | IC50: 5.7nM |
| JAK1 | IC50: 5.9nM |
| TYK2 | IC50: 53nM |
| JAK3 | IC50: >400nM |
| Chk2 | IC50: >1μM |
| c-Met | IC50: >10μM |
化学数据
| 目录号 | A11329 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 371.4 |
| Formula | C16H17N7O2S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 1187594-09-7 |
| Synonyms | INCB28050, LY3009104 |
| SMILES | CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3 |
溶解度
| In vitro (25°C) | DMSO | 65 mg/mL (175 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 4 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 26.93 mL | 134.63 mL | 269.25 mL |
| 0.5 mM | 5.39 mL | 26.93 mL | 53.85 mL |
| 1 mM | 2.69 mL | 13.46 mL | 26.93 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.39 mL |
*The above data is based on the productmolecular weight 371.4 . 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.
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