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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- Formule: C30H35N7O3
- Masse moléculaire:541.64
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Activité biologique
Description
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. Further protocols information, click here.
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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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Masse moléculaire 541.64
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Formule 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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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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SH-1092 Related Classifications
HY-183292 Related Classifications
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