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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-STX-478
STX-478

Chemical Structure : STX-478

CAS No.: 2883540-92-7

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STX-478 (STX478, STX 478)

货号: PC-21139Not For Human Use, Lab Use Only.

STX-478 (STX478) is a potent, mutant-selective, allosteric PI3Kα inhibitor with IC50 of 9.4 nM (PI3Kα H1047R), 14-fold selectivity over WT PI3Kα (IC50=131 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

STX-478 (STX478) is a potent, mutant-selective, allosteric PI3Kα inhibitor with IC50 of 9.4 nM (PI3Kα H1047R), 14-fold selectivity over WT PI3Kα (IC50=131 nM).
STX-478 is less potent against E542K (IC50=113 nM) and E545K (IC50=71 nM) helical domain mutants, but not alpelisib (Cat# PC-20590).
STX-478 also demonstrates exquisite kinome-wide selectivity against a panel 373 kinases representing approximately 70% of the human kinome at 10 uM, including PI3Kβ, PI3Kδ, and PI3Kγ isoforms, with only one exception of AurB kinase (IC50=1.6 µM).
STX-478 selectively inhibits the proliferation of cell lines with kinase-domain and helical-domain mutations compared with cells expressing WT PI3Kα.
STX-478 selectively targets PI3Kα activity and cell viability in PI3Kα mutant cells.
STX-478 (100 mg/kg QD) exhibits robust anti-tumor efficacy in PI3Kα-mutant tumors without metabolic dysregulation in mice.
STX-478 is efficacious across a panel of PI3Kα-mutant CDX and PDX 17 tumors, without evidence of insulin resistance.

物理化学性质&存储条件

分子量 401.30
分子式 C16H12F5N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-1-(2-aminopyrimidin-5-yl)-3-(1-(5,7-difluoro-3-methylbenzofuran-2-yl)-2,2,2-trifluoroethyl)urea

参考文献

1. Buckbinder L, et al. Cancer Discov. 2023 Aug 25:CD-23-0396.

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