New Building Blocks for August 2022_ChemScene -코아사이언스

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Building Blocks & Bioactive Molecules 전문제조사 ChemScene 수입/공급 업체 코아사이언스 입니다.

 

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As a receptor tyrosine kinase of insulin receptor (IR) subfamily, anaplastic lymphoma kinase (ALK) has been validated to play important roles in various cancers, especially anaplastic large cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastomas[1]. Currently, five small-molecule inhibitors of ALK, including Crizotinib, Ceritinib, Alectinib, Brigatinib and Lorlatinib, have been approved by the U.S. FDA against ALK-positive NSCLCs. To address the unmet need of the emergence of multiple combinations of acquired double ALK mutations, there are currently two 4G ALK TKIs (TPX-0131 and NVL-655) being developed. TPX-0131 has been designed with a novel compact macrocyclic structure and has shown preclinical potent inhibition of wildtype and numerous ALK mutations. NVL-655 is a novel brain-penetrant ALK-selective inhibitor created to overcome several limitations observed with currently available therapies and it started a phase 1/2 clinical trial on June 9, 2022[2-10].

A series of building blocks will be used as molecular fragments
in the design of ALK inhibitors.

 

[1] Journal of Medicinal Chemistry (2019), 62, 24, 10927-10954.
[2] Journal of Medicinal Chemistry (2019), 62, 10, 4915-4935.
[3] Journal of Medicinal Chemistry (2018), 61, 9, 4249-4255.
[4] European Journal of Medicinal Chemistry (2022), 238, 114493.
[5] Bioorganic & Medicinal Chemistry (2022), 66, 116794.
[6] Bioorganic & Medicinal Chemistry (2020), 28, 20, 115719.
[7] Bioorganic & Medicinal Chemistry (2019), 27, 20, 115051.
[8] Translational Oncology (2021), 14, 11, 101191.
[9] WO2021226208A2.
[10] WO2021226269A1.

 

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