EGFR-IN-133
EGFR-IN-133 (Compound 24) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. EGFR-IN-133 exhibits good pharmacokinetics characteristics with high oral exposure.
For research use only. We do not sell to patients.
- CAS No.: 2809982-26-9
- Formula: C27H29F2N7O3
- Molecular Weight:537.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
Description
IC50 & Target
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EGFR (WT) 0.1 nM (IC50) |
Chemical Information
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CAS No. 2809982-26-9
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Molecular Weight 537.56
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Formula C27H29F2N7O3
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SMILES
FC1=C2N3/C(NC2=CC(N[C@@H]4CCOC4)=C1)=N/C(C5=CC(F)=NC(C6=C(N(N=C6)C)OCCC[C@H](C3)C)=C5)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)