EGFR/CDK2-IN-5
EGFR/CDK2-IN-5 is a potent dual EGFR and CDK2 inhibitor with IC50s of 17.30 and 212.10 nM, respectively. EGFR/CDK2-IN-5 also inhibits EGFRT790M with an IC50 of 123.8 nM. EGFR/CDK2-IN-5 exhibits potent anticancer activity. EGFR/CDK2-IN-5 induces G1 and S cell cycle arrest and apoptosis, accompanied by increased levels of caspase-3/9 and Bax, as well as decreased Bcl-2 levels. EGFR/CDK2-IN-5 can be used for the research of cancers, such as lung cancer, breast cancer, and leukemia.
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- Formule: C31H32N4O3
- Masse moléculaire:508.61
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
CDK2 212.10 nM (IC50) |
EGFR 17.30 nM (IC50) |
EGFRT790M 123.8 nM (IC50) |
Caspase-9 |
Caspase-3 |
Bcl-2 |
Bax |
In Vitro
EGFR/CDK2-IN-5 (compound 7c) (48 h) exhibits broad-spectrum activity in a panel of cancer cells, displays potent activity against HCT-116 and LOX-IMVI with IC50s of 11.3 and 20.03 μM, while showing low cytotoxicity on normal cells WI-38 and Vero cells (IC50 > 50 μM) [1].
EGFR/CDK2-IN-5 (11.3-20.03 μM, 24 h) induces G1 phase arrest in HCT-116 and S phase arrest in LOX-IMVI cells, and induces apoptosis in both cells[1].
EGFR/CDK2-IN-5 (5.65 μM, 24 h) reduces the expression of EGFR, pEGFR, CDK2, and pCDK2 in HCT-116 cells.[1].
EGFR/CDK2-IN-5 (11.3 μM, 48 h) increases gene expression levels of caspase-3/9 and Bax, and BAX/Bcl-2 ratio, while decreasing Bcl-2 mRNA levels in HCT-116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116, LOX-IMVI
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Concentration:11.3 μM (HCT-116), 20.03 μM (LOX-IMVI)
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Incubation Time:24 h
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Result:Caused G1 phase arrest in HCT-116 and S phase arrest in LOX-IMVI.
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Cell Line:HCT-116
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Concentration:5.65 μM
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Incubation Time:24 h
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Result:Reduced the expression of EGFR, pEGFR, CDK2, and pCDK2 in HCT-116 cells.
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Cell Line:HCT-116, LOX-IMVI
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Concentration:11.3 μM (HCT-116), 20.03 μM (LOX-IMVI)
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Incubation Time:24 h
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Result:Induced apoptosis in n HCT-116 and LOX-IMVI cells.
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Cell Line:HCT-116
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Concentration:11.3 μM
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Incubation Time:48 h
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Result:Increased the mRNA levels of Bax, caspase-3, and caspase-9.
Increased BAX/Bcl-2 ratio.
Decreased Bcl-2 mRNA levels.
Chemical Information
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Masse moléculaire 508.61
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Formule C31H32N4O3
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SMILES
N#CC1=C(NCC2=CC(CN3CCN(C)CC3)=C(O)C(OC)=C2)OC(C4=CC=CC=C4)=C1C5=CC=CC=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR/CDK2-IN-5 Related Classifications
HY-180242 Related Classifications
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