1. Apoptosis
    Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. Apoptosis
    EGFR
  3. EGFR-IN-47

EGFR-IN-47 

Cat. No.: HY-143337
Handling Instructions

EGFR-IN-47 is a potent and orally active EGFRL858R/T790M/C797S inhibitor with an IC50 of 0.01 µM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC.

For research use only. We do not sell to patients.

EGFR-IN-47 Chemical Structure

EGFR-IN-47 Chemical Structure

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Description

EGFR-IN-47 is a potent and orally active EGFRL858R/T790M/C797S inhibitor with an IC50 of 0.01 µM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC[1].

IC50 & Target[1]

EGFRL858R/T790M/C797S

0.07 μM (IC50)

In Vitro

EGFR-IN-47 (compound 14aj) (72 h) shows anti-proliferative effects with IC50s of 0.013 µM, 2.972 µM, 1.031 µM for PC-9 (EGFRL858R/T790M/C797S), A432, A549 cells, respectively[1].
EGFR-IN-47 (0.01, 0.05, 0.25, 1 µM; 24 h) induces cell cycle attest at the G0/G1-phase[1].
EGFR-IN-47 (0.01, 0.05, 0.25 µM) induces cell deathvia apoptosis in a concentration-dependent manner[1].
EGFR-IN-47 (0.01, 0.05, 0.25, 1 µM) inhibits phosphorylation of the EGFR downstream mediators[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: PC-9 (EGFRL858R/T790M/C797S), A432, A549 cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferative effects with IC50s of 0.013 µM, 2.972 µM, 1.031 µM for PC-9 (EGFRL858R/T790M/C797S), A432, A549 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: PC-9 EGFRL858R/T790M/C797S cells
Concentration: 0.01, 0.05, 0.25, 1 µM
Incubation Time: 24 h
Result: Cells were arrest at the G0/G1-phase.

Apoptosis Analysis[1]

Cell Line: PC-9 EGFRL858R/T790M/C797S cells
Concentration: 0.01, 0.05, 0.25 µM
Incubation Time: 24 h
Result: Induced cell deathvia apoptosis in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: PC-9 EGFRL858R/T790M/C797S cells
Concentration: 0.01, 0.05, 0.25, 1 µM
Incubation Time:
Result: Inhibited phosphorylation of the EGFR downstream mediators.
In Vivo

EGFR-IN-47 (10, 20, 40 mg/kg; i.g.) shows anti-tumor effect with low toxicity[1].
EGFR-IN-47 (20 mg/kg for i.v.; 20 mg/kg for p.o.) shows an ideal oral bioavailability of 66.05%[1].
Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in Male Sprague-Dawley rats[1].

parameter iv (20 mg/kg) po (20 mg/kg)
AUC0-∞ (mg/Lh) 15.889 10.494
Cmax (mg/L) 6.845 0.77
Tmax (h) 0.083 6
F (%) 66.05
MRT0-∞ (h) 16.439 16.791
Vss (L/kg) 16.015 28.101
CL (L/h/kg) 1.272 2.151
t(1/2) (h) 8.922 11.154
Male Sprague-Dawley rats; 20 mg/kg for i.v.; 20 mg/kg for p.o.[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 weeks, BALB/c nude mice (PC-9 EGFRL858R/T790M/C797S cells )[1]
Dosage: 10, 20, 40 mg/kg (dissolved in 25% (v/v) PEG400 plus 5% DMSO)
Administration: I.g.
Result: Showed anti-tumor effect with low toxicity.
Animal Model: Male Sprague-Dawley rats[1]
Dosage: 20 mg/kg
Administration: I.v.; p.o.
Result: Showed an ideal oral bioavailability of 66.05%.
Molecular Weight

481.64

Formula

C29H35N7

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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EGFR-IN-47
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