STX-478, a Mutant-Selective, Allosteric Inhibitor bound to H1047R PI3Kalpha

STX-478, a Mutant-Selective, Allosteric Inhibitor bound to H1047R PI3Kalpha Descriptor: 1,2-ETHANEDIOL, N-(2-aminopyrimidin-5-yl)-N'-[(1R)-1-(5,7-difluoro-3-methyl-1-benzofuran-2-yl)-2,2,2-trifluoroethyl]urea, N~2~-{(4S,11aP)-2-[(4S)-4-(difluoromethyl)-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl}-L-alaninamide, ... Authors: Hilbert, B, Brooijmans, N, Buckbinder, L, St.Jean Jr, D.J. Deposit date: 2023-07-12 Release date: 2023-09-06 Last modified: 2023-11-08 Method: X-RAY DIFFRACTION (2.928 Å) Cite: STX-478, a Mutant-Selective, Allosteric PI3K alpha Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3K alpha-Mutant Xenografts. Cancer Discov, 13, 2023结合于H1047R突变型α型磷酸肌醇3-激酶（PI3Kα）的突变选择性变构抑制剂STX-478 描述项：1,2-乙二醇、N-(2-氨基嘧啶-5-基)-N'-[(1R)-1-(5,7-二氟-3-甲基-1-苯并呋喃-2-基)-2,2,2-三氟乙基]脲、N²-{(4S,11aP)-2-[(4S)-4-(二氟甲基)-2-氧代-1,3-恶唑烷-3-基]-5,6-二氢咪唑并[1,2-d][1,4]苯并氧氮杂卓-9-基}-L-丙氨酰胺…… 作者：Hilbert B、Brooijmans N、Buckbinder L、St.Jean Jr D.J. 入库日期：2023-07-12 发布日期：2023-09-06 最后修改日期：2023-11-08 实验方法：X射线衍射（分辨率2.928埃） 引用文献：《STX-478：一种突变选择性变构PI3Kα抑制剂，可规避代谢功能异常并改善PI3Kα突变异种移植瘤的治疗应答》，《癌症发现》（Cancer Discov），2023年，第13卷