EGFR-IN-175
EGFR-IN-175 is an orally active and selective EGFRL858R/T790M/C797S inhibitor with an IC50 of 18.94 nM. EGFR-IN-175 can induce cell apoptosis and cause G1 phase arrest. EGFR-IN-175 can downregulate p-EGFR, p-AKT, and p-ERK expression. EGFR-IN-175 can be used for the research of cancer, such as lung cancer.
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- Formule: C33H38N10O4S2
- Masse moléculaire:702.85
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
EGFRWT 125.9 nM (IC50) |
EGFRLR/TM 76.88 nM (IC50) |
EGFRLR/TM/CS 18.94 nM (IC50) |
In Vitro
EGFR-IN-175 (Compound M49) inhibits proliferation of BaF3-EGFRL858R/T790M/C797S, A431 and H1975 cells with IC50 values of 0.77, 5.11 and 5.94 μM[1].
EGFR-IN-175 (0.1-2.5 μM) dose-dependently downregulates phosphorylation levels of p-EGFR, p-AKT, and p-ERK in BaF3-TM cells[1].
EGFR-IN-175 (0.1-2.5 μM, 48 h) induces apoptosis and G1 phase arrest in BaF3-TM cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BaF3-TM cells
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Concentration:0.1, 1 and 2.5 μM
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Incubation Time:48 h
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Result:Increased apoptosis rate, reaching 69.68% at 2.5 μM.
Upregulated protein expression of Cleaved-PARP and Cleaved-Caspase-3.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BaF3-EGFRL858R/T790M/C797S xenograft BALB/c nude mice models[1]
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Dosage:30 mg/kg for i.p., 30 and 60 mg/kg for p.o
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Administration:Once a day for 14 days
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Result:Reduced tumor volume.
Reduced Ki67 and increased TUNEL-positive cells in tumors.
Downregulated p-EGFR.
Had no significant body weight loss and no toxicity to major organs.
Chemical Information
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Masse moléculaire 702.85
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Formule C33H38N10O4S2
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SMILES
O=C1C(C2=CC=CS2)=NC3=CN=C(NC4=CC=C(N5CCC(N6CCN(C)CC6)CC5)C=C4)N=C3N1C7=CN(S(=O)(C8CC8)=O)N=C7OC
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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-IN-175 Related Classifications
HY-178009 Related Classifications
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