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Bosutinib
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。
Bosutinib图片
CAS NO:380843-75-4
包装:10mg, 50mg, 100mg
包装与价格:
包装价格(元)
Free Sample (0.5-1 mg)电议
10mg电议
50mg电议
100mg电议

产品名称
SKI-606
产品介绍

生物活性

Bosutinib (SKI-606)是一种新型的Sarcoma/Abelson (Src/Abl)酪氨酸激酶双重抑制剂,其IC50分别为1.2 nM和1 nM。Bosutinib作用于Src比非Src家族激酶选择性高,IC50为1.2 nM,且有效抑制Src依赖的细胞增殖,IC50为100 nM。 Bosutinib 显著抑制Bcr-Abl阳性白血病细胞系KU812, K562, 和MEG-01 而不是 Molt-4, HL-60, Ramos, 和其他白血病细胞系的增殖,IC50分别为5 nM, 20 nM,和20 nM,比 STI-571更有效。与STI-571类似, Bosutinib 作用于Abl-MLV转化纤维,具有看增殖活性,IC50为 90 nM。


化学数据

分子量530.45
分子式C26H29Cl2N5O3
CAS号380843-75-4
纯度>99%
溶解性(25°C)DMSO
储存和运输条件2-8°C, protect from light
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系Abl-MLV, Rat 2, MEG-01, and K562 cell lines
方法cell lines were obtained from the American Type Culture Collection. The KU812 line was obtained from the European Collection of Cell Cultures. K562 and KU812 cell lines were maintained in RPMI 1640 supplemented with 10% FCS, glutamine, and nonessential amino acids (Life Technologies, Inc.). Rat 2 and Abl-MLV-transformed Rat 2 cells were maintained in high-glucose DMEM supplemented with 10% FCS. For proliferation assays, cells were exposed to compound for 72 h, and relative proliferation was measured with either 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium (Promega) or Cell-Glo (Promega). Anchorage-independent proliferation of Abl-MLV-transformed fibroblasts was measured in 96-well ultra-low binding plates (Costar) treated with Sigmacote (Sigma) to block residual cell attachment. Data analysis for IC50 calculations was performed with the LSW Data Analysis Package plug-in for Excel (Microsoft). For biochemical assays, cells were incubated with compound or DMSO alone for 4 h. Cells were prepared for FACS analysis as described in the CycleTest Plus DNA reagent kit (Becton Dickinson) and analyzed on a fluorescence-activated cell sorter flow cytometer.
浓度0~1μM
处理时间72h

动物实验
动物模型K562 Xenografts in nude mice
配制in a 0.2-ml suspension with 0.5% methocel/0.4% Tween 80.
剂量75 mg/kg twice a day
给药处理oral gavage

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM1.8852 mL9.426 mL18.8519 mL
5 mM0.377 mL1.8852 mL3.7704 mL
10 mM0.1885 mL0.9426 mL1.8852 mL