- One-step radiosynthesis of18F-IRS: A novel radiotracer targeting mutant EGFR in NSCLC for PET/CT imaging
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EGFR (epidermal growth factor receptor) targeted therapy has shown great success in clinical comparing with chemotherapy in EGFR mutation NSCLCs. Such as, gefitinib, first generation EGFR TKI, has obviously prolonged the FPS (progression free survival) of the subgroup of patients, but to those who did not get a certain mutation in EGFR kinase domain, the outcome is poor. In view of this situation, scientists have synthesized many radiotracers for selecting the right people by PET/CT imaging to NSCLC TKI therapy. In this study, we developed a novel PET radiotracer18F-IRS in one-step with a radio yield 20% (non-corrected), radiochemistry > 98.5%, specific activity > 105G Bq/μmol, the pharmacokinetics and capacity of the tracer binding to mutant EGFR were evaluated both in vitro and in vivo.
- Xiao, Zunyu,Song, Yan,Wang, Kai,Sun, Xilin,Shen, Baozhong
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- Development of a novel acetyl glucose-modified gefitinib derivative to enhance the radiosensitizing effect
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Various radiosensitizers are being developed to increase the radiation sensitivity of hypoxic cancer cells, which show resistance to radiation. Previously, we demonstrated that an acetyl glucose-modified nitroimidazole derivative showed a high radiosensit
- Yamahana, Hirari,Kunieda, Yukari,Tominaga, Masahide,Yamada, Hisatsugu,Uto, Yoshihiro
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- EGFR (epidermal growth factor receptor) kinase inhibitor and application thereof in preparation of anti-cancer drugs
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The invention discloses an EGFR (epidermal growth factor receptor) kinase inhibitor and application thereof in preparation of anti-cancer drugs, the EGFR kinase inhibitor can effectively improve EGFRTKI acquired drug resistance caused by SQSTM1 accumulati
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Paragraph 0270; 0274
(2020/11/23)
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- Fluorescent probe based on small molecule inhibitor as well as preparation method and application thereof
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The invention relates to a fluorescent probe based on a small-molecule inhibitor as well as a preparation method and application thereof, and belongs to the field of small-molecule labeled probes forfluorescence imaging. According to the invention, a smal
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Paragraph 0053-0055
(2020/09/20)
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- OXOINDOLINE DERIVATIVES AS PROTEIN FUNCTION MODULATORS
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The present invention provides chimeric compounds of formula (II) that modulate protein function, to restore protein homeostasis, including cytokine, aiolos, and/or ikaros activity, TNF-alpha activity, CKl-alpha activity and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as cytokine-mediated diseases, disorders, and conditions, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, organ transplant rejection, and cancer, are provided.
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Paragraph 0527
(2017/12/16)
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- Synthesis of [11C]Iressa as a new potential PET cancer imaging agent for epidermal growth factor receptor tyrosine kinase
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Iressa (Gefitinib) is an orally active inhibitor of epidermal growth factor receptor tyrosine kinase (EGFR-TK) involved in cell signal transduction processes critical to proliferation, apoptosis, repair, and angiogenesis of cancer cells. [11C]Iressa was first designed and synthesized as a new potential positron emission tomography (PET) cancer imaging agent for EGFR-TK in 30-40% radiochemical yield with 4.0-6.0 Ci/μmol specific activity at end of bombardment (EOB).
- Wang, Ji-Quan,Gao, Mingzhang,Miller, Kathy D.,Sledge, George W.,Zheng, Qi-Huang
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p. 4102 - 4106
(2007/10/03)
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- Facile synthesis of 7-amino anilinoquinazolines via direct amination of the quinazoline core
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The facile preparation of 4-(3-chloro-4-fluoroanilino)-6-alkoxy-7- aminoquinazolines from their corresponding 7-triflate and 7-fluoro precursors are highlighted.
- Harris, Craig S.,Kettle, Jason G.,Williams, Emma J.
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p. 7381 - 7384
(2007/10/03)
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