1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. EGFR-IN-48

EGFR-IN-48 

Cat. No.: HY-143445
Handling Instructions

EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.

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

EGFR-IN-48 Chemical Structure

EGFR-IN-48 Chemical Structure

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Description

EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFRd19/TM/CS, EGFRLR/TM/CS, EGFRWT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].

IC50 & Target

EGFRd19/TM/CS

0.193 nM (IC50)

EGFRLR/TM/CS

0.251 nM (IC50)

EGFRWT

10.4 nM (IC50)

In Vitro

EGFR-IN-48 (compound 23) (10 nM) shows anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively[1].
EGFR-IN-48 exhibits potent inhibitory activities against various clinically relevant EGFR mutants with IC50s of 10.4, 3.1, 0.9, 0.1, 0.2, 0.3, 0.2 nM for EGFRWT, EGFRLR, EGFRdel19, EGFRdel19/TM, EGFRLR/TM, EGFRLR/TM/CS, EGFRdrl19/TM/CS, respectively[1].

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

Cell Proliferation Assay[1]

Cell Line: BaF3EGFR del19/T790M/C797S, PC-9EGFR del19/T790M/C797S cells
Concentration: 10 nM
Incubation Time:
Result: Showed anti-proliferative activities against BaF3EGFR del19/T790M/C797S and PC-9EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively.
In Vivo

EGFR-IN-48 (2 mg/kg for i.v.; 10 mg/kg for o.p.) shows good oral bioavailability and high plasma exposure in CD-1 mouse[1]. Pharmacokinetic Parameters of EGFR-IN-48 in CD-1 mouse[1].

Route Dose (mg/kg) Vdss (L/kg) T1/2 (h) CL (L/h/kg) AUC0-last (h*ng/mL) Cmax (ng/mL) Tmax (h) F (%)
i.v. 2 0.7 3.3 2.4 13820.0
p.o. 10 33811.0 6600.0 0.5 48.9
CD-1 mouse; 2 mg/kg for i.v.; 10 mg/kg for o.p.[1].

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

Animal Model: CD-1 mouse[1]
Dosage:
Administration: 2 mg/kg for i.v.; 10 mg/kg for o.p.
Result: Showed good oral bioavailability and high plasma exposure.
Molecular Weight

800.75

Formula

C35H47BrN9O4PS

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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EGFR-IN-48
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HY-143445
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