An inhibitor of EGFR ex20ins
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STX-721

Item No. 44459

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(3-chloro-2-methoxyphenyl)amino]-2-[3-[2-[(2R)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]-2-methyl-2-pyrrolidinyl]ethynyl]-4-pyridinyl]-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one
CAS Number
2765525-82-2
Molecular Formula
C32H35ClN6O3
Formula Weight
587.1
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile:Water (1:1): Slightly soluble: 0.1-1 mg/ml
SMILES
O=C1C2=C(CCN1)NC(C3=CC=NC=C3C#C[C@](N4C(/C=C/CN(C)C)=O)(CCC4)C)=C2NC(C=CC=C5Cl)=C5OC
InChi Code
InChI=1S/C32H35ClN6O3/c1-32(14-7-19-39(32)26(40)10-6-18-38(2)3)15-11-21-20-34-16-12-22(21)28-29(27-24(36-28)13-17-35-31(27)41)37-25-9-5-8-23(33)30(25)42-4/h5-6,8-10,12,16,20,36-37H,7,13-14,17-19H2,1-4H3,(H,35,41)/b10-6+/t32-/m1/s1
InChi Key
UMSJPISUMQOUKS-LMZGTLAXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    STX-721 is an irreversible inhibitor of EGFR with an exon 20 insertion (ex20ins) mutation.1 It selectively inhibits the proliferation of Ba/F3 cells expressing EGFR exon20 A769_V770 insASV and EGFR exon20 D770_N771 insSVD (IC50s = 5.4 and 5.8 nM, respectively) over those expressing wild-type EGFR (IC50 = 127.365 nM). STX-721 (50 mg/kg once per day) induces tumor regression in a mouse xenograft model using NCI H2073 non-small cell lung cancer (NSCLC) cells expressing EGFR exon20 D770_N771 insSVD.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Milgram, B.C., Borrelli, D.R., Brooijmans, N., et al. Discovery of STX-721, a covalent, potent, and highly mutant-selective EGFR/HER2 exon20 insertion inhibitor for the treatment of non-small cell lung cancer. J. Med. Chem. 68(3), 2403-2421 (2025).