生物活性
Pacritinib (SB1518)是Janus激酶2（JAK2）和JAK2突变体JAK2V617F的口服生物利用抑制剂，无细胞试验中IC50分别为23和22 nM，具有潜在的抗肿瘤活性。Pacritinib与JAK2竞争ATP结合，这可能导致抑制JAK2活化，抑制JAK-STAT信号传导途径以及半胱天冬酶依赖性凋亡。
化学数据
| 目录号 | A12694 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 472.58 |
| Formula | C28H32N4O3 |
| 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. | 937272-79-2 |
| Synonyms | SB-1518; SB 1518 |
| SMILES | C1CCN(C1)CCOC2=C3COC/C=C/COCC4=CC=CC(=C4)C5=NC(=NC=C5)NC(=C3)C=C2 |
溶解度
| In vitro | DMSO | Warmed: 10 mg/mL (21.15 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
*<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 | 21.16 mL | 105.8 mL | 211.6 mL |
| 0.5 mM | 4.23 mL | 21.16 mL | 42.32 mL |
| 1 mM | 2.12 mL | 10.58 mL | 21.16 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.23 mL |
*The above data is based on the productmolecular weight 472.58. 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.
