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.
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- CAS. Nr.: 3052761-67-5
- Formel: C20H22FN3O7S
- Molecular Weight:467.47
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
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EGFRL858R 0.109 nM (IC50) |
EGFRC797S 0.75 nM (IC50) |
EGFRdel19 ＜0.05 nM (IC50) |
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.
Chemical Information
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CAS. Nr. 3052761-67-5
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Molecular Weight 467.47
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
EGFR-IN-167 Related Classifications
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