Bosutinib

产品编号: T0152 别名:

SKI-606,伯舒替尼

Bosutinib 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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CAS：380843-75-4

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.

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].

Cas No.

380843-75-4

分子式

C26H29Cl2N5O3

分子量

530.45

别名

SKI-606;伯舒替尼;Bosutinib

参考文献

[1]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.[2]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.[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.

引用文献

[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.

储存和溶解度

DMSO:53.1 mg/mL (100 mM)
Ethanol:13.3 mg/mL (25 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 Bosutinib 380843-75-4

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Keywords

inhibit Bosutinib cancer Bcr-Abl Src SKI-606 Oral Inhibitor Autophagy SKI 606 SKI606 伯舒替尼 Src/Abl tyrosine kinase inhibitor 380843-75-4

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Bosutinib

SKI-606,伯舒替尼

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