STX-478 is an allosteric PI3Kα inhibitor that selectively targets prevalent PI3Kα helical- and kinase-domain mutant tumors. STX-478 demonstrated robust efficacy in human tumor xenografts without causing the metabolic dysfunction observed with alpelisib. Combining STX-478 with fulvestrant and/or cyclin-dependent kinase 4/6 inhibitors was well tolerated and provided robust and durable tumor regression in ER+HER2− xenograft tumor models.
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名称 | STX-478 |
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Iupac 化学名称 | (R)-1-(2-aminopyrimidin-5-yl)-3-(1-(5,7-difluoro-3-methylbenzofuran-2-yl)-2,2,2-trifluoroethyl)urea |
同义词 | STX-478; STX 478; STX478; |
英文同义词 | STX-478; STX 478; STX478; |
分子式 | C16H12F5N5O2 |
分子量 | 401.29 |
Smile | NC1=NC=C(C=N1)NC(N[C@H](C2=C(C3=CC(F)=CC(F)=C3O2)C)C(F)(F)F)=O |
InChiKey | LGPNQALKGDDVBD-CYBMUJFWSA-N |
InChi | InChI=1S/C16H12F5N5O2/c1-6-9-2-7(17)3-10(18)12(9)28-11(6)13(16(19,20)21)26-15(27)25-8-4-23-14(22)24-5-8/h2-5,13H,1H3,(H2,22,23,24)(H2,25,26,27)/t13-/m1/s1 |
Cas号 | 2883540-92-7 |
相关CAS号 | 2883540-92-7 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 固体粉末 |
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纯度 | ≧98.0% |
存储 | 短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度 |
可溶性 | 溶于DMSO |
处理方式 | |
运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
海关编码 |
Targets | |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Kearney AL, Vasan N. A New Wave of PI3Kα Inhibitors. Cancer Discov. 2023 Nov 1;13(11):2313-2315. doi: 10.1158/2159-8290.CD-23-0945. PMID: 37909093.
2: Buckbinder L, St Jean DJ Jr, Tieu T, Ladd B, Hilbert B, Wang W, Alltucker JT, Manimala S, Kryukov GV, Brooijmans N, Dowdell G, Jonsson P, Huff M, Guzman-Perez A, Jackson EL, Goncalves MD, Stuart DD. STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts. Cancer Discov. 2023 Nov 1;13(11):2432-2447. doi: 10.1158/2159-8290.CD-23-0396. PMID: 37623743; PMCID: PMC10618743.