EGFR-IN-451
EGFR-IN-451 is an EGFR inhibitor with an IC50 value of 0.02 nM. EGFR-IN-451 also inhibits mutant EGFRL858R, EGFRT790M, and EGFRL858R/T790M with IC50 values of 0.26-34 nM. EGFR-IN-451 inhibits AKT and ERK activation and inhibits proliferation of EGFR-mutant cancer cells. EGFR-IN-451 can be used for the research of EGFR-driven cancer.
For research use only. We do not sell to patients.
- CAS No.: 220576-72-7
- Formula: C19H15N5O
- Molecular Weight:329.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All EGFR Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
EGFR 0.02 nM (IC50) |
EGFRL858R 0.26 nM (IC50) |
EGFRT790M 25 nM (IC50) |
EGFRL858R/T790M 34 nM (IC50) |
In Vitro
EGFR-IN-451 (Compound R14) (0.1-10000 nM) potently inhibits wild-type EGFR (IC50 = 0.02 nM), EGFRL858R (IC50 = 0.26 nM), EGFRT790M (IC50 = 25 nM), and EGFRL858R/T790M (IC50 = 34 nM) in a cell-free caliper mobility shift assay[1].
EGFR-IN-451 inhibits the viability of HCC827 cells (IC50 = 2.47 μM) and H1975 cells (IC50 = 18.07 μM) in an MTT assay[1].
EGFR-IN-451 (0.01-10 μM; 1-12 h) inhibits phosphorylated EGFR in HCC827 cells at 0.01 μM and in H1975 cells at 0.1, 1, and 10 μM, with sustained reduction of phosphorylated EGFR in HCC827 cells over 12 h, and inhibits P-AKT, P-ERK expression[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:HCC827 cells, H1975 cells
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:1, 4, 8, 12 h (time-course in HCC827 cells)
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Result:Inhibited phosphorylated EGFR in HCC827 cells at 0.01, 0.1 μM.
Reduced phosphorylated EGFR levels in HCC827 cells at 1, 4, 8, and 12 h post-treatment.
Inhibited phosphorylated EGFR in H1975 cells at 0.1, 1, and 10 μM.
Reduced P-AKT, P-ERK expression.
Chemical Information
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CAS No. 220576-72-7
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Molecular Weight 329.36
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Formula C19H15N5O
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SMILES
C=CC(NC1=CC2=C(N=CN=C2C=C1)NC3=CC4=C(C=C3)NC=C4)=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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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR-IN-451 Related Classifications
HY-116091 Related Classifications
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