STX-721 (STX721)

Chemical Structure : STX-721

CAS No.: 2765525-82-2

Catalog No.: 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	$178	In stock
5 mg	$378	In stock
10 mg	$588	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	587.12
Formula	C32H35ClN6O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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

References

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

STX-721 (STX721)

Biological Activity

Physicochemical Properties

References

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