生物活性
Cerdulatinib (PRT-062070)是多靶点酪氨酸激酶抑制剂，对JAK1/JAK2/JAK3/TYK2和Syk的IC50分别为12 nM/6 nM/8 nM/0.5 nM和32 nM。
Targets
| Target | Value |
| TYK2 | IC50: 0.5nM |
| MST1 | IC50: 4nM |
| ARK5 | IC50: 4nM |
| MLK1 | IC50: 5nM |
| Fms | IC50: 5nM |
| AMPK | IC50: 6nM |
| JAK2 | IC50: 6nM |
| JAK3 | IC50: 8nM |
| TBK1 | IC50: 10nM |
| MARK1 | IC50: 10nM |
| JAK1 | IC50: 12nM |
| PAR1B-a | IC50: 13nM |
| TSSK | IC50: 14nM |
| MST2 | IC50: 15nM |
| GCK | IC50: 18nM |
| JNK3 | IC50: 18nM |
| RSK2 | IC50: 20nM |
| RSK4 | IC50: 28nM |
| Syk | IC50: 32nM |
| Chk1 | IC50: 42nM |
| FLT4 | IC50: 51nM |
| FLT3 | IC50: 90nM |
| RET | IC50: 105nM |
| ITK | IC50: 194nM |
化学数据
| 目录号 | A14210 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 482 |
| Formula | C20H28ClN7O3S |
| 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. | 1369761-01-2 |
| Synonyms | PRT062070, PRT2070, PRT-2070 |
| SMILES | CCS(=O)(=O)N1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4CC4)C(=O)N.Cl |
溶解度
| In vitro (25°C) | DMSO | Warmed: 42 mg/mL (87.14 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 5% DMSO+corn oil | 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 20.75 mL | 103.73 mL | 207.47 mL |
| 0.5 mM | 4.15 mL | 20.75 mL | 41.49 mL |
| 1 mM | 2.07 mL | 10.37 mL | 20.75 mL |
| 5 mM | 0.41 mL | 2.07 mL | 4.15 mL |
*The above data is based on the productmolecular weight 482. 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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