CAS: 111358-88-4; (5S,6S,8R)-6-Hydroxy-6-(Hydroxymethyl)-5-Methyl-5,6,7,8,14,15-Hexahydro-13H-16-Oxa-4B,8A,14-Triaza-5,8-Methanodibenzo[b,H]Cycloocta[jkl]Cyclopenta[e]-As-Indacen-13-One

该化合物是一种针对多种强力体系的小型分子抑制剂, 包括JAK2,FLT3和Trk受体, 展示了针对这些群体的有力活动, 使其成为肿瘤学研究的候选体, 特别是血解恶性肿瘤和固态肿瘤的研究对象. 它的机制包括竞争性的ATP结合抑制, 干扰对细胞扩散和生存至关重要的下游信号信号路径. Lestaurtinib 在临床前研究中显示出希望, 因为它有能力抑制FLT3驱动的白血病和JAK2与宫颈性增生性失调有关. 化合物的特征是选择性和可逆性结合性, 有助于其在定向治疗发展中的调查效用. 继续进一步研究其药用动力学和药用动力学特征.

结构式图片

上下游产品

CAS号99533-80-9 (+)-抗生素 K 252A

合成工艺路线路线简述

    📜(+)-抗生素k252A置于锂硼氢体系中,用 四氢呋喃 用作溶剂,以81%的收率获得来他替尼
    参考文献:Synthesis And Kinase Inhibitory Activity Of 3'-(S)-Epi-K-252A
    标题:Synthesis And Kinase Inhibitory Activity Of 3'-(S)-Epi-K-252A
    摘要:The 3'-Epi Diastereomer Of K-252A Was Synthesized With The Goal Of Evaluating The Stereochemical Requirements Of The 3'-Sugar Alcohol On Kinase Inhibitory Activity. Inverting The 3'-Alcohol Resulted In A 20 Nm Inhibitor Of Vegfr2 And A 1 Nm Inhibitor Of Trka Tyrosine Kinase. (C) 2002 Elsevier Science Ltd. All Rights Reserved.
    Doi:10.1016/s0960-894X(02)00638-8

    海关参考信息

    专利信息


    专利号:US-10973847-B2
    优先权日:2017-06-30
    标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
    发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

    专利号:US-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    专利号:US-8828984-B2
    优先权日:2012-11-19
    标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection
    发明人:CHE CHI MING; ZOU TAOTAO
    权利人:UNIV HONG KONG; UNIV HONG KONG
    摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.

    专利号:US-10577387-B1
    优先权日:2018-08-09
    标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment
    发明人:CHE CHI MING; Fung Sin Ki; Chen tian feng
    权利人:UNIV HONG KONG
    摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

    专利号:US-11286271-B2
    优先权日:2018-07-31
    标 题 :Iridium (III) complexes containing N-heterocyclic carbene ligand, synthesis, and their use thereof in cancer treatment
    发明人:CHE CHI MING; LAM TSZ LUNG; TONG KA CHUNG
    权利人:UNIV HONG KONG
    摘要:Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

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    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Iyer R, Evans AE, Qi X, Ho R, Minturn JE, Zhao H, Balamuth N, Maris JM, Brodeur GM. Lestaurtinib enhances the antitumor efficacy of chemotherapy in murine xenograft models of neuroblastoma. Clin Cancer Res. 2010 Mar 1;16(5):1478-85. Epub 2010 Feb 23.
    2: Shabbir M, Stuart R. Lestaurtinib, a multitargeted tyrosine kinase inhibitor: from bench to bedside. Expert Opin Investig Drugs. 2010 Mar;19(3):427-36. Review. Epub 2010 Jan 11.
    4: Santos FP, Kantarjian HM, Jain N, Manshouri T, Thomas DA, Garcia-Manero G, Kennedy D, Estrov Z, Cortes J, Verstovsek S. Phase 2 study of CEP-701, an orally available JAK2 inhibitor, in patients with primary or post-polycythemia vera/essential thrombocythemia myelofibrosis. Blood. 2010 Feb 11;115(6):1131-6. Epub 2009 Dec 11. Epub 2009 Dec 10.

    合成参考文献


    参考文献:10.1016/j.bmc.2010.01.056
    摘要:Mashkani B, Griffith R, Ashman LK. Colony stimulating factor-1 receptor as a target for small molecule inhibitors. Bioorg Med Chem. 2010 Mar 01;18(5):1789–97. doi: 10.1016/j.bmc.2010.01.056.
    参考文献:10.1634/theoncologist.2011-0084
    摘要:Fathi AT, Chabner BA. FLT3 inhibition as therapy in acute myeloid leukemia: a record of trials and tribulations. Oncologist. 2011;16(8):1162–74.
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