2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR/C797S-IN-1

EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner.

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EGFR/C797S-IN-1 Chemical Structure

EGFR/C797S-IN-1 Chemical Structure

CAS No. : 2378188-21-5

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EGFR/C797S-IN-1 Related Antibodies

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Description

EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner[1].

IC50 & Target[1]

EGFRL858R/T790M/C797S

0.128 μM (IC50)

In Vitro

EGFR/C797S-IN-1 (compound 14d) (0-10 µM; 72 h) shows anti-proliferative activities with IC50s of 0.75, 0.09 µM for BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S, respectively[1].
EGFR/C797S-IN-1 (1-10000 nM; 24 h) decreases the expression of p-EGFR, p-AKT, p-ERK protein in a dose dependent manner[1].

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

EGFR/C797S-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: BaF3 cells with EGFRL858R/T790M/C797S and EGFR19del/T790M/C797S Mutations
Concentration: 0-10 µM
Incubation Time: 72 h
Result: Showed anti-proliferative activitie with IC50s of 0.75, 0.09 µM for BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S, respectively.

Western Blot Analysis[1]

Cell Line: BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S cells
Concentration: 1, 10, 100, 1000, 10000 nM
Incubation Time: 24 h
Result: Decreased the expression of p-EGFR, p-AKT. p-ERK protein in a dose dependent manner.
In Vivo

EGFR/C797S-IN-1 (10, 30 mg/kg; daily for 14 days) significantly decreases tumor growth in a dose-dependent manner in mouse[1].
Pharmacokinetic Parameters of EGFR/C797S-IN-1 in Male Sprague-Dawley rats[1].

Parameter i.v. (1 mg/kg) p.o. (10 mg/kg)
Tmax (h) 0.08±0 3.33±1.15
T1/2 (h) 1.97±0.14 3.89±0.42
Cmax (ng/mL) 69.57±6.78 7.43±1.17
AUC0-t (h*ng/mL) 65.48±5.55 61.12±6.23
AUC0-∞ (h*ng/mL) 67.98±5.56 62.15±6.36
CL-obs (L/h/kg) 14.78±1.19 --
Vss-obs (L/kg) 26.11±2.58 --
F (%) -- 9.33±0.95
Male Sprague-Dawley rats, 1 mg/kg iv ; 10 mg/kg po (dissolved in 5% DMSO, 10% Solutol and 85% Salinet with the concentration of 0.2 mg/mL for i.v. and 1 mg/mL for p.o.)[1].

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

Animal Model: SD male rats[1]
Dosage: 1 mg/kg for i.v.; 10 mg/kg for p.o.
Administration: i.v. or p.o.
Result: Displayed good biochemical activity and promising cellular activity.
Animal Model: BALB/c nude mice (BaF3-EGFR19del/T790M/C797S xenograft model)[1]
Dosage: 10, 30 mg/kg
Administration: I.p.; daily for 14 days
Result: Displayed an obvious suppressive effect of tumor growth, with the TGI at 51.36% and 67.95% at the dosage of 10 mg/kg and 30 mg/kg, respectively.
Molecular Weight

470.56

Formula

C28H30N4O3
CAS No.
SMILES

COC1=C(C=C2N=CN=C(C2=C1)NC3=CC=C(C=C3)OC4=CC=CC=C4)OCC5CCN(CC5)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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EGFR/C797S-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EGFR/C797S-IN-12378188-21-5EGFREpidermal growth factor receptorErbB-1HER1anti-proliferative activityanti-tumorBaF3 cellsp-EGFRp-AKTp-ERKInhibitorinhibitorinhibit

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