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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-HS-10375
HS-10375

Chemical Structure : HS-10375

CAS No.: 2567456-25-9

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HS-10375 (HS10375)

货号: PC-24741Not For Human Use, Lab Use Only.

HS-10375 is a potent, selective EGFR C797S tyrosine kinase inhibitor, shows potent inhibitory activity against EGFR C797S mutations (Del19/T790M/C797S, L858R/T790M/C797S, Del19/C797S, and L858R/C797S), and common and/or T790M mutations (Del19, T790M, L858R/T790M, and Del19/T790M) with IC50 < 1.5 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

HS-10375 is a potent, selective EGFR C797S tyrosine kinase inhibitor, shows potent inhibitory activity against EGFR C797S mutations (Del19/T790M/C797S, L858R/T790M/C797S, Del19/C797S, and L858R/C797S), and common and/or T790M mutations (Del19, T790M, L858R/T790M, and Del19/T790M) with IC50 < 1.5 nM.
HS-10375 shows weaker activity against wild type EGFR with IC50 of 9.1 nM.
HS-10375 binds deeply in the ATP-binding pocket and interacts with Met790 and Lys745 of EGFR T790M/C797S.
HS-10375 shows strong cell growth inhibition against Ba/F3 EGFR Del19/T790M/C797S cells with IC50 of 24.87 nM, but the IC50 of HS-10375 against EGFR-wildtype A431 cells is 148.93 nM.
HS-10375 potently inhibits EGFR Del19/T790M/C797S phosphorylation with an IC50 of 24 nM, at least 139 times more potently than gefitinib, afatinib, or osimertinib.
HS-10375 robustly inhibits EGFR signaling and phosphorylated EGFR (p-EGFR) at 100-1000 nM against Ba/F3 EGFR-L858R, L858R/C797S, L858R/T790M/C797S, Del19/C797S, and Del19/T790M/C797S, induces remarkable apoptosis against EGFR that harbored C797S.
HS-10375 (20 mg/kg, oral) showed dose-dependent inhibition of tumor growth in mice bearing PC9 EGFR-Del19/T790M/C797S, Ba/F3 EGFR-Del19/T790M/C797S, and Ba/F3 EGFR L858R/T790M/C797S xenografts or allografts.

物理化学性质&存储条件

分子量 701.60
分子式 C32H42BrN6O5P
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

(6-((5-bromo-2-((2-methoxy-4-(4-(3-(methoxymethyl)azetidin-1-yl)piperidin-1-yl)-5-methylphenyl)amino)pyrimidin-4-yl)amino)-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)dimethylphosphine oxide

参考文献

1. Zhan J, et al. J Transl Med. 2025 Jun 4;23(1):628.

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