EGFR-IN-167
EGFR-IN-1671 is a selective EGFR inhibitor with an IC50 of 0.19 nM. EGFR-IN-167 exhibits good potency against various EGFR mutants (IC50 = 0.109 nM, 0.75 nM and <0.05 nM against EGFR (L858R), EGFR (C797S) and EGFR (del19), respectively). EGFR-IN-1671 covalently engages the catalytically conserved lysine of EGFR in live mammalian cells. EGFR-IN-1671 demonstrates excellent anti-proliferative activity by inhibiting EGFR autophosphorylation. EGFR-IN-1671 can be used for the study of non-small-cell lung carcinomas (NSCLC), glioblastoma and many solid tumors.
For research use only. We do not sell to patients.
- CAS No.: 3052761-67-5
- Formula: C20H22FN3O7S
- Molecular Weight:467.47
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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]|
EGFRL858R 0.109 nM (IC50) |
EGFRC797S 0.75 nM (IC50) |
EGFRdel19 ＜0.05 nM (IC50) |
In Vitro
EGFR-IN-167 (Compound 26) (1 μM) exhibits excellent in vitro potency (IC50 = 35/< 1.8 nM)[1].
EGFR-IN-167 (1-100000 nM, 72 h) possesses good cytotoxic activity against both A431 and HCC827 cells (GI50 = 260 nM and 64 nM, respectively) and potently inhibits malignant cell proliferation (GI50 = 458 nM and 112.7 nM against H3255 (L858R) and Ba/F3 (C797S) cells, respectively)[1].
EGFR-IN-167 (0.01-10 μM, 4 h) results in a sustained inhibition of EGFR phosphorylation even after wash-out in in A431 and HCC827 cells[1].
EGFR-IN-167 possesses moderate microsomal stability (T1/2 = 29.6 min) in mouse liver
microsomes[1].
EGFR-IN-167 (10 μM) possesses favorable metabolic properties, with the inhibition ratios for the five main CYP isozymes (CYP1A2, 2C9, 2C19, 2D6 and 3A4) being <50%[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. 3052761-67-5
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Molecular Weight 467.47
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Formula C20H22FN3O7S
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SMILES
O=S(OC1=CC=CC(NC2=C3C=C(OCCOC)C(OCCOC)=CC3=NC=N2)=C1)(F)=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-167 Related Classifications
HY-176556 Related Classifications
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