QLH-11811
QLH-11811 is a mutant-selective EGFR tyrosine kinase inhibitor. QLH-11811 reversibly inhibits EGFR-19del/T790M/C797S and EGFR-L858R/T790M/C797S tyrosine kinase activity (IC50 = 2.6 nM and 3.1 nM, respectively), thereby overcoming C797S-mediated drug resistance. QLH-11811 exhibits weaker inhibitory activity against wild-type EGFR than against mutant EGFR variants. QLH-11811 can be used for research on advanced non-small cell lung cancer.
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- CAS No.: 2595202-02-9
- 화학식: C29H31BrN9O3P
- 분자량:664.49
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
제품 설명
In Vitro
QLH-11811 exhibits IC50 values of 2.6 nM and 3.1 nM against EGFR-19del/T790M/C797S-TK and EGFR-L858R/T790M/C797S-TK in Ba/F3 cell lines, respectively, and an IC50 of 61 nM against wild-type EGFR; in A431 cell lines, its IC50 against wild-type EGFR was 440 nM, demonstrating selectivity for mutant EGFR[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 2595202-02-9
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분자량 664.49
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화학식 C29H31BrN9O3P
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SMILES
CN1C=C(C=N1)C2=C(C=C(C(NC3=NC=C(C(NC4=CC=C5N=CC=NC5=C4P(C)(C)=O)=N3)Br)=C2)OC)N6CCOCC6
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)