EGFR/C797S-IN-1

Cat. No.: HY-152019: FAQs
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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.

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

EGFR/C797S-IN-1 Chemical Structure

CAS No. : 2378188-21-5

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

EGFR^{L858R/T790M/C797S}

0.128 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.09 μM Compound: 14d	Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR 19del/T790M/C797S triple mutant after 72 hrs by CCK-8 assay	[PMID: 36279692]
BaF3	IC₅₀	0.75 μM Compound: 14d	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant after 72 hrs by CCK-8 assay	[PMID: 36279692]

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-EGFR^{L858R/T790M/C797S}, BaF3-EGFR^{19del/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.

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-EGFR^{L858R/T790M/C797S}, BaF3-EGFR^{19del/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)
T_max (h)	0.08±0	3.33±1.15
T_1/2 (h)	1.97±0.14	3.89±0.42
C_max (ng/mL)	69.57±6.78	7.43±1.17
AUC_0-t (h*ng/mL)	65.48±5.55	61.12±6.23
AUC_0-∞ (h*ng/mL)	67.98±5.56	62.15±6.36
CL-obs (L/h/kg)	14.78±1.19	--
V_ss-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.

2378188-21-5

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

Handling Instructions (2659 KB)

References

[1]. Dou D, et al. Discovery and optimization of 4-anilinoquinazoline derivatives spanning ATP binding site and allosteric site as effective EGFR-C797S inhibitors. Eur J Med Chem. 2022 Dec 15;244:114856. [Content Brief]

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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