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Bosutinib

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 Chemical Structure
Bosutinib, CAS 380843-75-4
规格 价格/CNY 货期 数量
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
其他形式的 Bosutinib:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: Bosutinib (T0152)
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选择批次  
纯度: 99.9%
纯度: 99.84%
纯度: 99%
纯度: 99%
纯度: 99%
纯度: 98.98%
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生物活性
化学信息
存储 & 溶解度
参考文献
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
100 mM 0.0189 mL 0.0943 mL 0.1885 mL 0.4713 mL

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TargetMol Library Books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.

TargetMol Library Books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.
Cenisertib Radotinib BGG463 BCR-ABL-IN-8 Rigosertib Berbamine dihydrochloride Silybin B Ponatinib

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 药物功能重定位化合物库 EMA 上市药物库 抑制剂库 激酶抑制剂库 FDA 上市激酶抑制剂库 抗癌活性化合物库 抗癌上市药物库 抗癌临床化合物库 抗癌药物库

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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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