2378188-21-5

2378188-21-5 structure

Name: EGFR/C797S-IN-1
Chemical Name: EGFR/C797S-IN-1
CAS Number: 2378188-21-5
Molecular Formula: C₂₈H₃₀N₄O₃
Molecular Weight: 470.56
Catalog: Signaling Pathways JAK/STAT Signaling EGFR
Create Date: 2023-01-18 10:09:31
Modify Date: 2024-04-08 10:45:15
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].

Name	EGFR/C797S-IN-1

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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Target	EGFRL858R/T790M/C797S:0.128 μM (IC50)
In Vitro	EGFR/C797S-IN-1 (compound 14d) (0-10 µM; 72 h) 显示抗增殖活性，对BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S 的 IC50 值分别为 0.75、0.09 µM [1]。 EGFR/C797S-IN-1 (1-10000 nM; 24 h) 以剂量依赖性降低 p-EGFR、p-AKT、p-ERK 蛋白的表达[1]。 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；每日一次，持续 14 天) 呈剂量依赖性显著降低小鼠体内的肿瘤生长[1]。 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.
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.

Molecular Formula	C₂₈H₃₀N₄O₃
Molecular Weight	470.56

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