STX-721

STX-721 is an irreversible inhibitor of EGFR with an exon 20 insertion (ex20ins) mutation. It selectively inhibits the proliferation of Ba/F3 cells expressing EGFR exon20 A769_V770 insASV and EGFR exon20 D770_N771 insSVD (IC50s = 5. and 5. nM, respectively) over those expressing wild-type EGFR (IC50 = 127. 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. 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: 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. Storage: -20°C. Stability: > 4 years.