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Bosutinib

产品编号 T0152 CAS 380843-75-4

别名: 伯舒替尼, SKI-606

Bosutinib (SKI-606) 是一种合成的喹诺酮衍生物和双激酶抑制剂，靶向 Abl 和 Src 激酶的 IC50分别为 1 nM 和 1.2 nM。

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Bosutinib, CAS 380843-75-4

规格	价格/CNY	货期
1 mg	￥ 113	现货
5 mg	￥ 229	现货
10 mg	￥ 372	现货
25 mg	￥ 533	现货
50 mg	￥ 689	现货
100 mg	￥ 892	现货
200 mg	￥ 1,490	现货
500 mg	￥ 2,380	现货
1 mL * 10 mM (in DMSO)	￥ 413	现货

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其他形式的 Bosutinib:

Bosutinib hydrate
现货
Bosutinib D8
询价

选择批次

纯度: 99.9%

纯度: 99.84%

纯度: 99%

纯度: 98.98%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Bosutinib (SKI-606) is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.
靶点活性	Abl:1 nM (cell free), Src:1.2 nM (cell free)
体外活性	Bosutinib has the antiproliferative activity against three different Bcr-Abl-positive leukemia cell lines (KU812, K562, and MEG-01). Bosutinib inhibited 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. Inhibition of proliferation by Bosutinib is associated with cell cycle arrest and cell death. Treatment with Bosutinib at 100 nM for 24 h (KU812) or 48 h (K562) resulted in a reduction of S and G2-M phase cells and an increase of cells with a DNA content of less than 2N. Treatment with Bosutinib at 100 nm also led to PARP degradation after 48 h. The potent antiproliferative activity of Bosutinib against CML lines was not a general property for leukemia cell lines. Molt-4, HL-60, Ramos, and other leukemia cell lines were unaffected by Bosutinib at concentrations less than 1 μM [2].
体内活性	Bosutinib (30/25 mg/kg, b.i.d) reduces tumor growth in unstaged and staged Src-transformed fibroblast mouse xenograft models. Bosutinib (100 mg/kg) also induces complete tumor regression in a K562 mouse xenograft model when administered once per day for five days [2].
激酶实验	The Src kinase activity is measured in an ELISA format. Src (3 units/reaction), reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4) and cdc2 substrate peptide are added to various concentration of Bosutinib and incubated at 30 °C for 10 minutes. The reaction is started by the addition of ATP to a final concentration of 100 μM, incubated at 30 °C for 1 hour and stopped by addition of EDTA. Instructions from the manufacturer are followed for subsequent steps. The Abl kinase assay is performed in a DELFIA solid phase europium-based detection assay format. Biotinylated peptide (2 μM) is bound to streptavidin-coated microtitration plates for 1.5 hours in 1 mg/mL ovalbumin in PBS. The plates are washed for 1 hour with PBS/0.1% Tween 80, followed by a PBS wash. The kinase reaction is incubated for 1 hour at 30°C. Abl kinase (10 units) is mixed with 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4, 1% DMSO, 1 mM HEPES (pH 7.0), 200 μg/mL ovalbumin and various concentration of Bosutinib. The reaction is stopped with EDTA at a final concentration of 50 mM. The reaction is monitored with Eu-labeled phosphotyrosine antibody and DELFIA enhancement solution [2].
细胞实验	Cells are exposed to various concentrations of Bosutinib for 72 hours. Anchorage-independent proliferation of Abl-MLV-transformed fibroblasts is measured in 96-well ultra-low binding plates treated with Sigmacote to block residual cell attachment. Cell proliferation is measured with MTS or Cell-Glo. For the determination of cell cycle or cell death, cells are prepared for FACS analysis in the CycleTest Plus DNA reagent kit and analyzed on a fluorescence-activated cell sorter flow cytometer [2].
动物实验	K562 cells were suspended to 50 million cells/ml in Matrigel (1 volume of cells with 1 volume of cold Matrigel). Nude female mice 6–7 weeks of age were given injections of 0.2 ml of this suspension. Tumors were staged for 10 days, at which time they entered the growth phase. At this time, the compound was administered by oral gavage in a 0.2-ml suspension with 0.5% methocel/0.4% Tween 80 [2].

别名	伯舒替尼, SKI-606
分子量	530.45
分子式	C26H29Cl2N5O3
CAS No.	380843-75-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 53.1 mg/mL (100 mM)

Ethanol: 13.3 mg/mL (25 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	1.8852 mL	9.426 mL	18.8519 mL	47.1298 mL
	5 mM	0.377 mL	1.8852 mL	3.7704 mL	9.426 mL
	10 mM	0.1885 mL	0.9426 mL	1.8852 mL	4.713 mL
	20 mM	0.0943 mL	0.4713 mL	0.9426 mL	2.3565 mL
DMSO	50 mM	0.0377 mL	0.1885 mL	0.377 mL	0.9426 mL
DMSO	100 mM	0.0189 mL	0.0943 mL	0.1885 mL	0.4713 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Boschelli DH, et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J Med Chem. 2001 Nov 8;44(23):3965-77. 2. Golas JM, et al. SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice. Cancer Res. 2003 Jan 15;63(2):375-81. 3. Golas JM, et al. SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res. 2005 Jun 15;65(12):5358-64.

文献引用

1. Cheng S, Jin P, Li H, et al. Evaluation of CML TKI Induced Cardiovascular Toxicity and Development of Potential Rescue Strategies in a Zebrafish Model. Frontiers in Pharmacology. 2021: 2866. 2. Yan H, Wu W, Hu Y, et al.Regorafenib inhibits EphA2 phosphorylation and leads to liver damage via the ERK/MDM2/p53 axis.Nature Communications.2023, 14(1): 2756.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Bosutinib 380843-75-4 Angiogenesis Autophagy Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl Src inhibit cancer SKI606 SKI 606 Oral Inhibitor 伯舒替尼 SKI-606 Src/Abl tyrosine kinase inhibitor inhibitor

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Bosutinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords