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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3052761-67-5
- Formule: C20H22FN3O7S
- Masse moléculaire:467.47
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform EGFR
More
Activité biologique
|
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
-
CAS No. 3052761-67-5
-
Masse moléculaire 467.47
-
Formule C20H22FN3O7S
-
SMILES
O=S(OC1=CC=CC(NC2=C3C=C(OCCOC)C(OCCOC)=CC3=NC=N2)=C1)(F)=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR-IN-167 Related Classifications
HY-176556 Related Classifications
Powered by Bioz