EGFR/VEGFR2-IN-10
EGFR/VEGFR2-IN-10 is a selective EGFR, VEGFR2 and COX2 inhibitor with IC50s of 8.5, 68 and 158 nM, respectively. EGFR/VEGFR2-IN-10 induces G1-phase cell cycle arrest in MCF-7 cells. EGFR/VEGFR2-IN-10 increases the Bax/Bcl-2 ratio, upregulates caspase-8, and elevates caspase-9 protein levels, confirming activation of the intrinsic apoptotic pathway. EGFR/VEGFR2-IN-10 demonstrates exceptional therapeutic potential by simultaneously inhibiting tumor proliferation, angiogenesis, and inflammation pathways while maintaining a favorable selectivity profile. EGFR/VEGFR2-IN-10 can be used as a research tool for cervical, liver, colon, and breast cancer studies.
For research use only. We do not sell to patients.
- Formula: C25H18BrN5O2S
- Molecular Weight:532.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Help & FAQs
Biological Activity
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EGFR 8.5 nM (IC50) |
VEGFR2 68 nM (IC50) |
COX-2 158 nM (IC50) |
Caspase 8 |
Caspase 9 |
EGFR/VEGFR2 IN 10 exhibits potent antitumor activity against Hela, HepG2, HCT 116, MCF 7 with IC₅₀ values of 4.93, 2.34, 6.07, and 3.35 μM, and high selectivity indices (SI) of 16.86, 11.78, 8.00, and 6.50 respectively, respectively, showing cytotoxicity toward normal WI 38 cells (IC₅₀ = 39.45 μM)[1].
EGFR/VEGFR2-IN-10 (3.35 μM, 48 h) blocks cell cycle progression at the G1 checkpoint and induces programmed cell death in MCF-7 cells[1].
EGFR/VEGFR2 IN 10 (3.35 μM, 48 h) exerts a selective anticancer mechanism in MCF 7 breast cancer cells by potently inducing apoptosis (both early and late stages) without causing necrosis or associated inflammatory responses, and simultaneously enhances proapoptotic signals while suppressing anti apoptotic defenses to overcome apoptosis resistance[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:3.35 μM
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Incubation Time:48 h
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Result:Disrupted MCF-7 cell cycle kinetics.
Resulted in an accumulation of cells in G1 phase.
Produced a modest reduction in S phase cell population.
Increased sub-G1 phase cells from 0.35 % to 0.57 %.
Suppressed the G2/M phase cell population to 14.17%, compared to 20.27% in the untreated control.
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Cell Line:MCF-7 breast cancer cells
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Concentration:3.35 μM
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Incubation Time:48 h
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Result:Decreased the viable cell population from 96.58% to 58.25 %.
Increased early apoptotic cells remarkably from 1.49% to 22.52%.
Increased late apoptotic cells rising from 1.13% to 18.47%.
Decreased the necrotic cell slightly from 0.80% to 0.76%.
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Cell Line:MCF-7 cells
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Concentration:3.35 μM
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Incubation Time:48 h
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Result:Increased the Bax/Bcl-2 ratio by 5.11-fold (p < 0.001) in MCF-7, this shift was driven by a 2.71-fold upregulation (p < 0.01) of the pro-apoptotic protein Bax and a concomitant 47% reduction (p < 0.05) in the anti-apoptotic protein Bcl-2.
Induced a 2.90-fold increase (p < 0.001) in caspase-8 and a 1.72-fold increase (p < 0.05) in caspase-9 gene expression, confirming the initiation of the caspase cascade.
Chemical Information
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Molecular Weight 532.41
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Formula C25H18BrN5O2S
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SMILES
[H]C1=CC=C(C=C1)N2C(C3=CC=CC=C3N=C2SCC(C4=C(N(N=N4)C5=CC=C(C=C5)Br)C)=O)=O
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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/VEGFR2-IN-10 Related Classifications
HY-179485 Related Classifications
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