SH-1092
SH-1092 is an orally active EGFR inhibitor with an IC50 of 0.96 nM against EGFRT790M/L858R and an IC50 of 6.1 nM against wild-type EGFR. SH-1092 exhibits anticancer activity against non-small cell lung cancer. SH-1092 can be used in studies related to non-small cell lung cancer.
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- Fòrmula: C30H35N7O3
- Peso molecular:541.64
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
EGFRL858R/T790M 0.96 nM (IC50) |
EGFR (WT) EGFR nM (IC50) |
In Vitro
SH-1092 potently inhibits EGFRT790M/L858R with an IC50 of 0.96 nM; it also inhibits wild-type EGFR with an IC50 of 6.1 nM, exhibits moderate selectivity for the mutant form, and shows weak inhibitory effects on IGF1R and INSR[1].
SH-1092 (0.1 nM-10 μM; 72 h) inhibits the proliferation of H1975 (EGFRT790M/L858R) cells and A431 (wild-type EGFR) 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 (EGFR T790M/L858R mutant) non-small cell lung cancer cell line, A431 (EGFR wild-type) non-small cell lung cancer cell line
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Concentration:0.1 nM-10 μM
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Incubation Time:72 h
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Result:Inhibited the growth of H1975 cells with an IC50 of 8 nM.
Inhibited the growth of A431 cells with an IC50 of 362 nM.
Parmacokinetics
In Vivo
SH-1092 (10-50 mg/kg; p.o.; daily; 14 days) exhibits dose-dependent, significant antitumor activity against EGFRT790M/L858R mutant H1975 NSCLC xenografts in female BALB/c nude mice with low acute toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Significantly inhibited A431 xenograft tumor growth in a dose-dependent manner.
Did not change mouse body weight significantly during treatment, indicating low acute toxicity.
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Animal Model:BALB/c nude (female)[1]
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Dosage:10 mg/kg; 25 mg/kg; 50 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Significantly inhibited H1975 xenograft tumor growth in a dose-dependent manner.
Did not change mouse body weight significantly during treatment, indicating low acute toxicity.
Chemical Information
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Peso molecular 541.64
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Fòrmula C30H35N7O3
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SMILES
C=CC(NC1=CC(NC2=NC=C(C)C(C3=CN4C5=C3C=CC=C5OCC4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SH-1092 Related Classifications
HY-183292 Related Classifications
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