Bosutinib hydrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Bosutinib（水合物）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 active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range.IC50: 314 nmol/L (Csk, Src family protein tyrosine kinases); IC50: 2.4 nmol/L(Abl kinase).

Bosutinib (hydrate) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range.Cell Proliferation AssayCell Line:The leukemic Bcr-Abl+ cell lines (KCL22, K562, KU812, and Lama84)Concentration:0.1 μmol/LIncubation Time:72 hResult:Inhibited several human CML derived cell lines with IC50 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. Animal Model:KU812CM L xenograft model Dosage:75 mg/kg twice daily or 150 mg/kg once dailyAdministration: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 xenograftsDosage: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.

——

Others

Other Targets

——

——

——

918639-08-4

548.46

C26H31Cl2N5O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (182.33 mM)

CN1CCN(CC1)CCCOC2=C(C=C3C(NC4=CC(OC)=C(C=C4Cl)Cl)=C(C=NC3=C2)C#N)OC.O

——

(-20℃)

With Ice Pack

≥ 2 years