CAS: 1047644-62-1; N-((S)-1-Amino-3-(3-Fluorophenyl)Propan-2-yl)-5-Chloro-4-(4-Chloro-1-Methyl-1H-Pyrazol-5-yl)Thiophene-2-Carboxamide

该化合物是一种针对AKT(Portein kinase B)的强大和选择性的小型分子抑制器,它是PI3K/AKT/mtor信号信号路径的一个关键组成部分,它经常在各种癌症中出现衰竭,使Afuresertib成为有希望的肿瘤研究的治疗对象.该复合物显示出AKT异形,特别是AKT1,AKT2和AKT3的高度特异性,在固体肿瘤的临床前型模型中表现出了效力.其特性精致的药理动力和抑制下游信号分子的能力有助于其克服对其他目标疗法的抗药性.Afuresertib在治疗卵巢,乳房和前列腺恶性肿瘤时的应用受到调查,PI3K/AKT路径活化非常普遍.

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上下游产品

5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-N-{(1S)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-1-[(3-fluorophenyl)methyl]ethyl}-2-thiophenecarboxamide methyl 5-chloro-4-iodo-2-thiophenecarboxylate methyl 5-chloro-4-(1-methylpyrazol-5-yl)-2-thiophenecarboxylate 5-Chlorothiophene-2-carboxylic acidN-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydr°Chloride

合成工艺路线路线简述

    📜Tert-Butyl [(1S)-1-(3-Fluorobenzyl)-2-Hydroxyethyl]Carbamate置于盐酸,偶氮二甲酸二异丙酯,N,N-二异丙基乙胺,三苯基膦,Pybrop,肼体系中,用 四氢呋喃,甲醇,二氯甲烷 用作溶剂,化学反应生成Gsk-2110183C无结构图
    参考文献:Afuresertib: Protein Kinase B (Pkb) Inhibitor Oncolytic
    标题:Afuresertib: Protein Kinase B (Pkb) Inhibitor Oncolytic
    摘要:The Phosphatidylinositol 3-Kinase (513K)/akt/mammallan Target Of Raparnycin (Mtor) Signaling Pathway Plays Key Roles In Cellular Proliferation And Survival. Mutations And Alterations In This Signal Transduction Pathway Have Been Described In A Variety Of Solid And Hematopoietic Malignancies,Which May Contribute To Perpetuation Of The Disease In A Number Of Ways. Increasing Interest In Targeting Particular Facets Of This Signaling Cascade Has Led To The Development Of A Number Of Novel Anticancer Agents,Including Afuresertib (Gsk-2770783),An Orally Bioavailable Pan-Inhibitor Of The Rac-Alpha Serine/threonine Protein Kinase,Also Referred To As Protein Kinase B Or Proto-Oncogene C-Akt. The Present Review Summarizes The Preclinical And Pharmacological Aspects Of Afuresertib And Early Clinical Experience.
    Doi:10.1358/dof.2014.039.08.2177902

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Uko NE, Güner OF, Matesic DF, Bowen JP. Akt Pathway Inhibitors. Curr Top Med Chem. 2020;20(10):883-900. doi: 10.2174/1568026620666200224101808.
    2022:1832241. doi: 10.1155/2022/1832241.
    3: Cho H, Abshire ET, Popp MW, Pröschel C, Schwartz JL, Yeo GW, Maquat LE. AKT constitutes a signal-promoted alternative exon-junction complex that regulates nonsense-mediated mRNA decay. Mol Cell. 2022 Aug 4;82(15):2779-2796.e10. doi: 10.1016/j.molcel.2022.05.013. Epub 2022 Jun 7.
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