Bosutinib (hydrate) 是一种口服Src/Abl酪氨酸激酶抑制剂，IC50分别为1.2 nM和1 nM。

Bosutinib (hydrate) is an oral Src/Abl tyrosine kinase inhibito with IC 50 of 1.2 nM and 1 nM, respectively [1].

Bosutinib (hydrate) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC 50 values in the low nanomolar range [2]. Cell Proliferation Assay [2] Cell Line: The leukemic Bcr-Abl+ cell lines (KCL22, K562, KU812, and Lama84) Concentration: 0.1 μmol/L Incubation Time: 72 h Result: Inhibited several human CML derived cell lines with IC 50 values ranging from 1 to 20 nmol/L.

Bosutinib (hydrate) (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) has activity against human KU812 xenografts in nude mice. Bosutinib (hydrate) (150 mg/kg; once daily, 5 days weekly) has activity against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts [2]. Animal Model: KU812CM L xenograft model [2] Dosage: 75 mg/kg twice daily or 150 mg/kg once daily Administration: Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) Result: Had the therapeutic activity and produced a dose- and schedule-dependent weight loss. Animal Model: Syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts [2] Dosage: 150 mg/kg Administration: Bosutinib (150 mg/kg; once daily, 5 days weekly) Result: Decreased the rate of tumor growth and prolonged event-free survival of mice.

918639-08-4

C26H31Cl2N5O4

548.46

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years