Bosutinib (SKI-606)
Bosutinib (SKI-606) structure
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Common Name | Bosutinib (SKI-606) | ||
|---|---|---|---|---|
| CAS Number | 380843-75-4 | Molecular Weight | 530.446 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 649.7±55.0 °C at 760 mmHg | |
| Molecular Formula | C26H29Cl2N5O3 | Melting Point | 116-120ºC | |
| MSDS | Chinese USA | Flash Point | 346.7±31.5 °C | |
| Symbol |
GHS07 |
Signal Word | Warning | |
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Src Kinase Is the Connecting Player between Protein Kinase A (PKA) Activation and Hyperpolarization through SLO3 Potassium Channel Regulation in Mouse Sperm.
J. Biol. Chem. 290 , 18855-64, (2015) Plasma membrane hyperpolarization is crucial for mammalian sperm to acquire acrosomal responsiveness during capacitation. Among the signaling events leading to mammalian sperm capacitation, the immediate activation of protein kinase A plays a pivotal role, pr... |
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In vitro and in vivo identification of ABCB1 as an efflux transporter of bosutinib.
J. Hematol. Oncol. 8 , 81, (2015) Bosutinib is a recently approved ABL inhibitor. In spite of the well-documented effectiveness of BCR-ABL inhibitors in treating chronic myeloid leukemia, development of resistance is a continuous clinical challenge. Transporters that facilitate drug uptake an... |
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A simple method for the determination of Bosutinib in rat plasma by UPLC-MS/MS.
J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 1004 , 93-7, (2015) In this work, a simple, sensitive and fast ultra performance liquid chromatography with tandem mass spectrometry (UPLC-MS/MS) method was developed and validated for the quantitative determination of bosutinib in rat plasma. Plasma samples were processed with ... |
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Quantitative high-throughput identification of drugs as modulators of human constitutive androstane receptor.
Sci. Rep. 5 , 10405, (2015) The constitutive androstane receptor (CAR, NR1I3) plays a key role in governing the transcription of numerous hepatic genes that involve xenobiotic metabolism/clearance, energy homeostasis, and cell proliferation. Thus, identification of novel human CAR (hCAR... |
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Pilot Trial of Selecting Molecularly Guided Therapy for Patients with Non-V600 BRAF-Mutant Metastatic Melanoma: Experience of the SU2C/MRA Melanoma Dream Team.
Mol. Cancer Ther. 14 , 1962-71, (2015) Targeted therapies and immunotherapies have led to significant improvements in the treatment of advanced cancers, including metastatic melanoma. However, new strategies are desperately needed to overcome therapeutic resistance to these agents, as well as to i... |
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Cancer chemotherapy and cardiac arrhythmias: a review.
Drug Saf. 38(2) , 129-52, (2015) Cardiovascular toxicity is a potential complication of cancer chemotherapy (CC) that increases the morbidity and mortality of cancer patients. Cardiac arrhythmias have been reported as an adverse effect of many chemotherapeutic drugs, including novel targeted... |
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SRC family kinase inhibitors antagonize the toxicity of multiple serotypes of botulinum neurotoxin in human embryonic stem cell-derived motor neurons.
Neurotox. Res. 27(4) , 384-98, (2015) Botulinum neurotoxins (BoNTs), the causative agents of botulism, are potent inhibitors of neurotransmitter release from motor neurons. There are currently no drugs to treat BoNT intoxication after the onset of the disease symptoms. In this study, we explored ... |
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Imatinib reduces cholesterol uptake and matrix metalloproteinase activity in human THP-1 macrophages.
Pharmacol. Rep. 68 , 06-Jan, (2016) Imatinib mesylate (Glivec®, formerly STI-571) is a selective tyrosine kinase inhibitor used for the treatment of chronic myeloid leukemia and gastrointestinal stromal tumors. However, there are reports suggesting that imatinib could be atheroprotective by low... |
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Phase 2 study of bosutinib, a Src inhibitor, in adults with recurrent glioblastoma.
J. Neurooncol. 121(3) , 557-63, (2015) Tumor cell infiltration is a major mechanism of treatment escape in glioblastoma. Src is an intracellular tyrosine kinase that mediates tumor cell motility and invasiveness. We evaluated the efficacy and safety of bosutinib, a tyrosine kinase inhibitor that p... |
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SRC-mediated EGF receptor activation regulates ozone-induced interleukin 8 expression in human bronchial epithelial cells.
Environ. Health Perspect. 123(3) , 231-6, (2015) Human exposure to ozone (O3) results in pulmonary function decrements and airway inflammation. The mechanisms underlying these adverse effects remain unclear. Epidermal growth factor receptor (EGFR) plays an important role in the pathogenesis of lung inflamma... |