STX-721 (STX721)

Chemical Structure : STX-721

CAS No.: 2765525-82-2

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货号: PC-21322Not For Human Use, Lab Use Only.

STX-721 is a potent, selective, irreversible, orally active inhibitor of EGFR/HER2 ex20ins mutants with IC50 of 5.4 nM and 5.8 nM for cellular Ba/F3 EGFR ex20insASV and insSVD mutant activity, respectively.

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1 mg	￥1780	In stock
5 mg	￥3780	In stock
10 mg	￥5880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

STX-721 is a potent, selective, irreversible, orally active inhibitor of EGFR/HER2 ex20ins mutants with IC50 of 5.4 nM and 5.8 nM for cellular Ba/F3 EGFR ex20insASV and insSVD mutant activity, respectively.

STX-721 demonstrates excellent selectivity vs WT-EGFR (24- and 22-fold, respectively), approaching osimertinib's level of selectivity for EGFR L858R/T790 M (29-fold).

STX-721 retains good biochemical EGFR ex20insNPG activity, selectivity over WT-EGFR, and excellent kinome selectivity (S(10) at 3 μM = 0.027).

STX-721 (30 mg/kg BID) resulted in 52% TGI, while 100 mg/kg QD afforded 100% tumor regression over 7 days of dosing in mouse Ba/F3 EGFR ex20insASV allograft model, with minimal (<6%) body weight loss in the animals.

STX-721 dosed orally results in selective regression of EGFR ex20insSVD tumor xenografts relative to EGFR WT control xenografts.

物理化学性质&存储条件

分子量	587.12
分子式	C32H35ClN6O3
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,E)-3-((3-chloro-2-methoxyphenyl)amino)-2-(3-((1-(4-(dimethylamino)but-2-enoyl)-2-methylpyrrolidin-2-yl)ethynyl)pyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one

参考文献

1. Milgram BC, J Med Chem. 2025 Jan 17. doi: 10.1021/acs.jmedchem.4c02377.

STX-721 (STX721)

生物&药学活性

物理化学性质&存储条件

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STX-721 (STX721)

生物&药学活性

物理化学性质&存储条件

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