Bosutinib hydrate

立即咨询

Bosutinib hydrate

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

918639-08-4

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

SKI-606 hydrate

产品介绍

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。

生物活性

Bosutinib (hydrate) is an oral Src/Abl tyrosine kinase inhibito withIC₅₀of 1.2 nM and 1 nM, respectively^[1].

IC₅₀& Target

IC50: 314 nmol/L (Csk, Src family protein tyrosine kinases); IC50: 2.4 nmol/L(Abl kinase).

体外研究
(In Vitro)

Bosutinib (hydrate) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, withIC₅₀values 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 withIC₅₀values ranging from 1 to 20 nmol/L.

体内研究
(In Vivo)

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.

Clinical Trial

分子量

548.46

Formula

C₂₆H₃₁Cl₂N₅O₄

CAS 号

918639-08-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.