HER2-IN-23 

HER2-IN-23 is a selective HER2 inhibitor. HER2-IN-23 reduces in total HER2 expression rather than in phosphorylated HER2 (p-HER2). HER2-IN-23 reduces cyclin D1 level and stimulates PARP cleavage. HER2-IN-23 can be used for the study of HER2-positive breast cancer^[1].

HER2-IN-23 (Compound 4o) (0.4-25 μM, 72 h) shows moderate antiproliferative activity against HER2-positive cells (such as BT474 (IC₅₀ = 10.5 μM), A431 (IC₅₀ = 9.9 μM), and HCC1954 (IC₅₀ = 8.5 μM)), but exhibits lower activity against HER2-negative cells (such as MDA-MB-231 (IC₅₀ = 19.7 μM) and MCF7 (IC₅₀ = 12.8 μM))^[1].
HER2-IN-23 (1 μM) inhibits HER2 kinase by 84% at a concentration of 1 μM, while showing low or no inhibition against other kinases (such as EGFR, HER4, IGF1R, etc.)^[1].
HER2-IN-23 (10 μM, 24 h) significantly reduces total HER2 expression in A431 cells, but phosphorylated HER2 (p-HER2) shows no significant change; simultaneously, cyclin D1 expression is almost completely inhibited, and an increase in PARP cleavage is observed^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

398.81

C₂₂H₁₆ClFO₄

O=C1C(C2=CC=C(OCC3=CC=CC(F)=C3)C(Cl)=C2)=COC4=C1C(CCC4)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Rubinov DB, et al. A facile method for the preparation of 7,8-dihydro-4H-chromene-4,5(6H)-diones as non-aromatic cycle A analogs of isoflavones and their evaluation as antiproliferative agents. Bioorg Chem. 2025 Oct;165:108960.  [Content Brief]