Bosutinib是一种新型的双重Src/Abl抑制剂，在无细胞试验中IC50分别为1.2 nM 和 1 nM。Bosutinib也可通过阻滞p-ERK、p-S6和p-STAT3的磷酸化来有效地降低PI3K/AKT/mTOR、MAPK/ERK和JAK/STAT3信号通路的活性。Bosutinib可促进自噬。
| CAS No. | 380843-75-4 |
| 生物活性 | Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively. |
| 分子式 | C26H29Cl2N5O3 |
| 分子量 | 530.45 |
| 储存条件 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | DMSO : ≥ 46 mg/mL (86.72 mM) |
| 体内研究 | Bosutinib (50-150 mg; p.o.; once a day for 5 days) remaines tumor free at 150 mg/kg, whereas at the lower doses, some relapse occurs over a 40-day period in K562 Xenografts in Nude Mice. |
| 体外研究 | Bosutinib (100 nM; 24/48 hours) results in a reduction of S and G2-M phase cells and an increase of cells with a DNA content of less than 2N. Bosutinib inhibits the proliferation of all three cell lines, with IC50s ranging from 5 nM in the KU812 line to 20 nM for the K562 and MEG-01 cell lines. Bosutinib (10-500 nM; 4 hours) ablates tyrosine phosphorylation of STAT5 at 25 nM. |
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