EGFR T790M/L858R-IN-2

EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity[1].

Product Specifications

CAS Number

[2955607-40-4]

UNSPSC

12352005

Target

Apoptosis; EGFR

Type

Reference compound

Related Pathways

Apoptosis; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/egfr-t790m-l858r-in-2.html

Purity

99.66

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

C=CC(NC1=CC=CC(NC2=C3C=C(F)C=CC3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O

Molecular Formula

C28H28FN7O

Molecular Weight

497.57

References & Citations

[1]Pei J, et al. Design, Synthesis, and Antitumor Activity of Potent and Selective EGFR L858R/T790M Inhibitors and Identification of a Combination Therapy to Overcome Acquired Resistance in Models of Non-small-cell Lung Cancer. J Med Chem. 2023 Apr 27;66 (8) :5719-5752.