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Submit ReviewBosutinib is a dual inhibitor of Abl and Src kinases (IC50 = 1.2 nM for Src in an enzymatic assay). Displays antiproliferative activity against chronic myelogenous leukemia (CML) cells and decreases the motility and invasion of breast cancer cell lines. Also exhibits potent antiproliferative activity in anchorage-independent, Src-transformed rat fibroblasts (IC50 = 100 nM). Displays selectivity for Src over non-Src family kinases such as growth factor receptor tyrosine kinases.
Sold for research purposes under agreement from Pfizer Inc.
Bosutinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 530.45 |
公式 | C26H29Cl2N5O3 |
储存 | Store at +4°C |
纯度 | ≥99% |
CAS Number | 380843-75-4 |
PubChem ID | 5328940 |
InChI Key | UBPYILGKFZZVDX-UHFFFAOYSA-N |
Smiles | ClC1=CC(Cl)=C(OC)C=C1NC3=C(C#N)C=NC2=CC(OCCCN4CCN(C)CC4)=C(OC)C=C23 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 53.05 | 100 | |
ethanol | 13.26 | 25 |
以下数据基于产品分子量 530.45。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.89 mL | 9.43 mL | 18.85 mL |
5 mM | 0.38 mL | 1.89 mL | 3.77 mL |
10 mM | 0.19 mL | 0.94 mL | 1.89 mL |
50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
参考文献是支持产品生物活性的出版物。
Boschelli et al (2001) Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J.Med.Chem. 44 3965 PMID: 11689083
Golas et al (2003) 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. 63 375 PMID: 12543790
Golas et al (2005) SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res. 65 5358 PMID: 15958584
Vultur et al (2008) SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells. Mol.Cancer.Ther. 7 1185 PMID: 18483306
If you know of a relevant reference for Bosutinib, please let us know.
关键词: Bosutinib, Bosutinib supplier, dual, inhibitors, inhibits, abl, src, kinases, antiproliferative, SKI-606, Src, Kinases, Abl, Kinase, 4361, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Bosutinib 的部分引用包括:
Levinson and Boxer (2012) Structural and spectroscopic analysis of the kinase inhibitor bosutinib and an isomer of bosutinib binding to the Abl tyrosine kinase domain. PLoS One 7 e29828 PMID: 22493660
Marina et al (2021) Machine learning identifies molecular regulators and therapeutics for targeting SARS-CoV2-induced cytokine release. Mol Syst Biol 17 e10426 PMID: 34486798
Levinson (2014) A conserved water-mediated hydrogen bond network defines bosutinib's kinase selectivity. Nat Chem Biol 10 127 PMID: 24292070
Mark et al (2013) Calcium-activated chloride channel ANO1 promotes breast cancer progression by activating EGFR and CAMK signaling. Proc Natl Acad Sci U S A 110 E1026-34 PMID: 23431153
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