EGFR/PARP-1-IN-1 

EGFR/PARP-1-IN-1 is a dual EGFR and PARP-1 inhibitor with IC₅₀ values of 64 nM and 12 nM, respectively. EGFR/PARP-1-IN-1 binds to the ATP-binding pocket of EGFR and interacts with the catalytic domain of PARP-1, inhibiting kinase and enzymatic activity via hydrogen bond formation with key residues in both targets. EGFR/PARP-1-IN-1 induces apoptosis through the endogenous mitochondrial pathway, arrests the cell cycle at the G2 phase, and inhibits cell proliferation. EGFR/PARP-1-IN-1 can be used for research on triple-negative breast cancer^[1].

EGFR/PARP-1-IN-1 (0.01-100 μM; 48 h) potently inhibits MDA-MB-231 cell viability with an IC₅₀ of 1.27 μM, and exhibits high selectivity for cancer cells over normal breast epithelial cells^[1].
EGFR/PARP-1-IN-1 (1.27 μM; 48 h) induces a 7.16-fold increase in apoptotic cell death and a 4.9-fold increase in necrotic cell death in MDA-MB-231 cells^[1].
EGFR/PARP-1-IN-1 (1.27 μM; 48 h) induces cell cycle arrest at the G2 phase and increases the Sub-G1 population, indicating DNA damage and apoptosis in MDA-MB-231 cells^[1].
EGFR/PARP-1-IN-1 (1.27 μM; 48 h) upregulates pro-apoptotic genes and downregulates the anti-apoptotic gene Bcl-2, primarily via intrinsic apoptotic pathways in MDA-MB-231 cells^[1].

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

538.30

C₂₃H₁₄BrF₂N₇O₂

O=C(N/N=C1C(N(CC2=CN(C3=CC=C(F)C(F)=C3)N=N2)C4=C\1C=C(Br)C=C4)=O)C5=CC=NC=C5

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• [1]. Alshams MA, et al. Design and synthesis of novel isatin-isoniazidhydrazone hybrid-based 1,2,3-triazoles as dual EGFR/PARP-1 inhibitors and apoptosis inducers in breast cancer cells. Bioorg Chem. 2026;176:109859.