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Revumenib CAS# 2169919-21-3 N-乙基-2-[[4-[7-[[[反式-4-[(乙磺酰基)氨基]环己基]甲基]-2,7-二氮杂螺[3.5]非-2-基]-5-嘧啶基]氧基]-5-氟-N-(1-甲基乙基)苯甲酰胺
Revumenib (SNDX-5613) is a potent, orally bioavailable small-molecule inhibitor of the menin–KMT2A (MLL) protein-protein interaction critical in certain acute leukemias. In preclinical binding studies...
Design of Potent Menin-KMT2A Interaction Inhibitors with Improved In Vitro ADME Properties and Reduced hERG AffinityBy: Chapsal, Bruno D. ; et alACS Medicinal Chemistry Letters (2025), 16(2), 224-233
Paltusotine CAS# 2172870-89-0 3-(4-(4-氨基哌啶-1-基)-3-(3,5-二氟苯基)喹啉-6-基)-2-羟基苯腈
Paltusotine (CRN00808) is a potent, selective, orally bioavailable non-peptide somatostatin receptor 2 (SST2) agonist with an EC₅₀ of ~0.25 nM and >4,000-fold selectivity over other somatostatin subty...
Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 AgonistBy: Zhao, Jian ; et alACS Medicinal Chemistry Letters (2023), 14(1), 66-74
Lenacapavir CAS# 2189684-44-2 HIV-1衣壳抑制剂GS-6207
Lenacapavir (GS-6207) is a first-in-class, long-acting capsid inhibitor targeting HIV-1. In preclinical studies, it bound the HIV-1 capsid protein with subnanomolar affinity (Kd ~0.43 nM), disrupting ...
Clinical targeting of HIV capsid protein with a long-acting small moleculeBy: Link, John O.; et alNature (London, United Kingdom) (2020), 584(7822), 614-618
Ixabepilone CAS# 219989-84-1 伊沙匹隆
Ixabepilone (also known as azaepothilone B, or BMS-247550) is an orally bioavailable microtubule inhibitor. Ixabepilone was a semisynthetic analogue of epothilone B with antineoplastic activity. Ixabe...
Synthesis of epothilones, intermediates and analogs for use in treatment of cancers with multidrug resistant phenotype; Danishefsky, Samuel J.; Lee, Chul Bom; Chappell, Mark; Stachel, Shawn; Chou, Ting-chao; Assignee Sloan-Kettering Institute for Cancer Research, USA; 2001; Patent Information; Sep 07, 2001; WO 2001064650 A2
Elexacaftor CAS# 2216712-66-0
Elexacaftor, also known as VX-445 and WHO 11180, is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore Phe508del CFTR protein function in patien...
Haseltine, Eric L.; Moskowitz, Samuel; Robertson, Sarah; Waltz, David. Methods of treatment for cystic fibrosis. Assignee Vertex Pharmaceuticals Incorporated, USA. WO 2019018395. (2019).
Retapamulin CAS# 224452-66-8 瑞他莫林
Retapamulin, also known as SB-275833, is a newer topical agent of pleuromutilin class approved by the Food and Drug Administration for treatment of impetigo in children. It has been demonstrated to ha...
Breen, Gary Francis; Forth, Michael Anthony; Kopelman, Susan Shumei Hu; Muller, Francis Xavier; Sanderson, Francis Dominic. Process for preparation of mutilin derivatives and their salts as antibacterial agents. Assignee Glaxo Group Limited, UK. WO 2005023257. (2005).
Sotorasib CAS# 2252403-56-6 6-氟-7-(2-氟-6-羟基苯基)-1-[4-甲基-2-(1-甲基乙基)-3-吡啶基]-4-[(2S)-2-甲基-4-(1-氧代-2-丙烯-1-基)-1-哌嗪基]-吡啶并[2,3-d]嘧啶-2(1H)-酮
Sotorasib (AMG 510) is a first-in-class, selective, covalent inhibitor of KRAS^G12C^. In preclinical biochemical assays, it irreversibly bound the mutant cysteine residue in KRAS^G12C^, locking it in ...
Discovery of a Covalent Inhibitor of KRASG12C(AMG 510) for the Treatment of Solid TumorsBy: Lanman, Brian A. ; et alJournal of Medicinal Chemistry (2020), 63(1), 52-65
Maralixibat Chloride CAS# 228113-66-4 氯马昔巴特
Maralixibat chloride (LUM001) is a potent, selective, orally bioavailable inhibitor of the ileal bile acid transporter (IBAT/ASBT). In preclinical studies, it blocked bile acid reuptake in the termina...
Stereoselective Synthesis of Maralixibat via VO(acac)2/Schiff Base-Catalyzed Asymmetric Oxidation of Its Sulfide IntermediateBy: Peng, Ziyu; et alJournal of Organic Chemistry (2024), 89(19), 14510-14514
Lapatinib CAS# 231277-92-2 拉帕替尼
Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the E...
Zhang, Yaling; Zhang, Ying; Liu, Juan; Chen, Li; Zhao, Lijun; Li, Baolin; Wang, Wei. Synthesis and in vitro biological evaluation of novel quinazoline derivatives. Bioorganic & Medicinal Chemistry Letters. Volume 27. Issue 7. Pages 1584-1587. 2017
Nifurtimox CAS# 23256-30-6 硝呋替莫
Nifurtimox is a 5-nitrofuran and is used to treat diseases caused by trypanosomes including Chagas disease and sleeping sickness. It is given by mouth and not by injection. Nifurtimox is now in a Phas...
A continuous flow generator of acetyl nitrate for the synthesis of nitrofuran-based pharmaceuticalsBy: Hellwig, Hubert; et alChemRxiv (2025), 1-9
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