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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-Dyr726
Dyr726

Chemical Structure : Dyr726

CAS No.:

Dyr726

货号: PC-24357Not For Human Use, Lab Use Only.

Dyr726 is a potent, selective and brain-penetrant inhibitor of PI3Kα with IC50 of 3.6 nM, >1,000-fold selective against the β and γ-PI3K isoforms.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Dyr726 is a potent, selective and brain-penetrant inhibitor of PI3Kα with IC50 of 3.6 nM, >1,000-fold selective against the β and γ-PI3K isoforms.
Dyr726 also inhibits common PI3Kα activating mutants, E542K, E545K, and H1047R with IC50s of 5nM, 3.8nM, and 15.7nM respectively.
Dyr726 inhibits the oncogenic PI3K-AKT-mTOR signaling pathway with complete ablation of phospho-AKT, phospho-PRAS40, and phospho-S6K in primary patient derived GBM6 cells.
Dyr726 is a very potent inhibitor of the type III RTKs PDGFRA/B, KIT and FLT3, inhibits PDGFRA at 62nM, PDGFRB at 76nM, KIT at 13nM, and FLT3 at 55nM.
Dyr726 targets oncogenic gain-of-function mutants of PDGFRA and PI3Kα.
Dyr726 is a very potent inhibitor of the DYRK and CLK family of CMGC kinases with biochemical IC50s of less than 100 nM for all isoforms except CLK3 (277 nM).
Dyr726 kills WNT-dependent cancer organoids and extends survival of tumour mice in vivo.

物理化学性质&存储条件

分子量
分子式
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

参考文献

1. Vasudha Tandon, et al. bioRxiv. 2025 Mar 29:2025.03.26.645490.

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