EGFR-IN-44
EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC50 of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers.
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- Formule: C27H29ClN6O2S
- Masse moléculaire:537.08
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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
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Activité biologique
IC50: 0.26 nM (EGFR T790M/L858R), 1.33 nM (EGFR L858R), 4.11 nM (EGFR)[1]
EGFR-IN-44 (Compound 6a) (0-10 µM, 72 h) shows anti-proliferative activities against tumor cell lines[1].
EGFR-IN-44 binds to the ATP binding site of EGFR[1].
EGFR-IN-44 (0-10 nM, 48 h) induces H1975 cell apoptosis via the mitochondrial pathway, arrests cell cycle in G0/G1 phase, and suppresses cell migration[1].
EGFR-IN-44 (0-10 nM, 48 and 72h) shows hypotoxicity against normal cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975 (EGFRT790M/L858R), PC9 (EGFRdel19), and H292 (EGFRWT)
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Concentration:0-10 µM
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Incubation Time:72 h
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Result:Showed anti-proliferative activities with IC50 values of 0.0022 ± 0.001, 0.0048 ± 0.001, and 4.499 ± 0.057 µM against H1975, PC9, and H292 cells, respectively.
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Cell Line:H1975
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Concentration:1, 5, and 10 nM
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Incubation Time:48 h
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Result:Effectively induced cell apoptosis in a dose-dependent manner. Resulted in 33.7%, 52.4%, and 56.2% apoptosis at 1, 5, and 10 µM, respectively, compared to 5.81% apoptosis in the control group.
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Cell Line:H1975
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Concentration:5, 10, and 25 nM
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Incubation Time:48 h and 72 h
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Result:Dose-dependently upregulated the expression levels of the proapoptotic proteins Bad and Bax and downregulated the expression level of the antiapoptotic protein Bcl-2. Sufficiently reduced the phosphorylation of EGFR and AKT.
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Cell Line:H1975
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Concentration:5 nM
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Incubation Time:0, 12, 24, or 48 h
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Result:Exhibited a significant increase in the G0/G1 cell population and a dramatic decrease in G2/M phase.
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Cell Line:LO2, HK2, HLF, and 293A
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Concentration:0.1, 1, 5, and 10 µM
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Incubation Time:48 h and 72 h
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Result:Showed hypotoxicity with IC50 values of 7.247, 4.586, 3.787, and 2.925 µM against LO2, HK2, HLF, and 293A cells, respectively. The cell morphology was changed compared to the control.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c nude mice (5 weeks old, 18 - 20 g), H1975 xenograft model[1]
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Dosage:25 mg/kg
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Administration:Intragastric administration, daily, 7 days
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Result:Showed strong tumor inhibition (TGI = 90.24%) without obvious toxicity.
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Animal Model:Male Sprague–Dawley (SD) rats[1]
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Dosage:1 mg/kg and 5 mg/kg
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Administration:Intravenous injection and oral administration (Pharmacokinetic Analysis)
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Result:In Vivo PK parameters of EGFR-IN-44 [1]
Parameters
Dose(mg/kg)EGFR-IN-44
5 (po)
1 (iv)t1/2 (h) 8.60 ± 1.8 1.42 ± 0.1 Tmax (h) 4.00 ± 0.002 / Cmax (ng/mL) 80.40 ± 2.7 / Vz F_pred (L/kg) 220.80 ± 41.2 6.83 ± 08 AUC0-t (H.ng/mL) 490.41 ± 29.9 291.91 ± 38.2 AUC0-∞ (H.ng/mL) 491.02 ± 44.2 295.76 ± 38.8 MRT0-last (h) 7.93 ± 0.8 1.35 ± 01 CL (mL/h/kg) 17.79 ± 3.9 3.12 ± 0.4 F(%) 33.57 ± 5.9 /
F = (AUC0-inf-PO × DOSEIV)/(AUC0-inf-IV × DOSE PO)*100%.
Chemical Information
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Masse moléculaire 537.08
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Formule C27H29ClN6O2S
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SMILES
C=CC(NC1=CC(NC2=NC(C3=CSC4=CC=CC=C43)=C(C=N2)Cl)=C(C=C1N(CCN(C)C)C)OC)=O
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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-44 Related Classifications
HY-145844 Related Classifications
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