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.
For research use only. We do not sell to patients.
- Formula: C23H14BrF2N7O2
- Molecular Weight:538.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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EGFR 64 nM (IC50) |
PARP-1 12 nM (IC50) |
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.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:1.27 μM
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Incubation Time:48 h
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Result:Increased total apoptotic cell death to 13.1% and necrotic cell death to 8.74%, representing a 7.16-fold increase in apoptosis and a 4.9-fold increase in necrosis compared to untreated control cells (total apoptosis 1.83%, necrosis 1.78%).
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:1.27 μM
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Incubation Time:48 h
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Result:Reduced G1 phase to 33.06% and S phase to 18.76%, increased G2 phase to 31.48%, and increased Sub-G1 phase to 11.37% compared to untreated control cells (G1 phase 44.41%, S phase 27.39%, G2 phase 26.48%, Sub-G1 phase 0.47%).
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:1.27 μM
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Incubation Time:48 h
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Result:Increased expression of pro-apoptotic genes: P53 (9.87-fold), Bax (4.69-fold), Caspase-3 (5.66-fold), Caspase-8 (1.2-fold), and Caspase-9 (7.69-fold).
Decreased expression of the anti-apoptotic gene Bcl-2 by 0.24-fold.
Chemical Information
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Molecular Weight 538.30
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Formula C23H14BrF2N7O2
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SMILES
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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR/PARP-1-IN-1 Related Classifications
HY-183373 Related Classifications
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