类似于ML323,USP1的N160与KSQ-4279在氢键距离范围内(图1F)。D751和D752催化天冬氨酸所在的 β 转角被KSQ-4279的吡唑并[3,4-d]嘧啶基团推动,相对于无抑制剂的USP1发生轻微位移(图2)。在ML323中,嘧啶的甲基取代基也推动了这个β转角,但程度更大,并且还位移了S753。为容纳KSQ-4279的甲氧基取代基,F101稍微...
KSQ Therapeutics 与罗氏就KSQ-4279达成全球许可协议。KSQ-4279是FIC、强效和选择性的USP1小分子抑制剂,目前正处于治疗实体瘤的1期临床试验中。根据协议,罗氏将在2024年全面负责KSQ-4279的进一步开发。
描述 KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP.KSQ-4279 has anticancer activity and is used in the study of non-small cell lung cancer, osteosarcoma, ovarian, breast, glioblastoma, bladder, uterine and pancreatic cancers. 存储条件 store at low temperature | Powder: -20°C ...
KSQ-4279, a first-in-class USP1 inhibitor shows strong combination activity in BRCA mutant cancers with intrinsic or acquired resistance to PARP inhibitorsdoi:10.1016/s0959-8049(22)00900-5L. CadzowP. GokhaleS. GanapathyP. SullivanS. Nayak...
靶点 ubiquitin carboxyl-terminal hydrolase 1 (USP1) 作用机制 USP1抑制剂 药品简介 -- 研发机构 KSQ Therapeutics ;Roche 最高研发阶段 全球: I期临床 中国: 临床前 审评审批类型 -- 外置链接 -- KSQ-4279 CAS Number: -- Molecular Formula: -- Molecular Weight: -- 了解药物更多情报 登录查...
KSQ-4279 (USP1-IN-1, Formula I) 是USP1 和 PARP 的抑制剂。 名称和标识符 InChIKey KCBWAFJCKVKYHO-UHFFFAOYSA-N Inchi 1S/C27H25F3N8O/c1-15(2)37-13-20(27(28,29)30)35-24(37)18-6-4-16(5-7-18)12-38-25-19(11-34-38)10-31-23(36-25)21-22(17-8-9-17)32-14-33-26(...
英文同义词 1H-Pyrazolo[3,4-d]pyrimidine, 6-(4-cyclopropyl-6-methoxy-5-pyrimidinyl)-1-[[4-[1-(1-methylethyl)-4-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]methyl]-;KSQ-4279;USP1-IN-1;6-(4-cyclopropyl-6-methoxy-pyrimidin-5-yl)-1-[[4-[1-isopropyl-4-(trifluoromethyl)imidazol-2-yl]...
KSQ Therapeutics, Inc. announced today it has entered into a worldwide license and collaboration agreement with Roche for the development and commercialization of KSQ-4279.
中文名KSQ-4279 英文名KSQ-4279 中文别名 英文别名KSQ 4279; KSQ4279;Usp1-IN-1; 分子式C27H25F3N8O分子量534.54 用途 生物活性KSQ-4279 is a USP1 and PARP inhibitor. KSQ-4279 showed anti-proliferative effects in a subset of cell lines, often characterized by the presence of homologous recombinati...
化合物KSQ-4279 T60039Product IntroductionBioactivity英文名: KSQ-4279描述: KSQ-4279 (USP1-IN-1)是 USP1 和 PARP 的抑制剂。KSQ-4279 具有抗癌活性,可用于研究非小细胞肺癌、骨肉瘤、卵