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: 2025-08-26 06:37:53
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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[1].
| Name | EGFR/C797S-IN-1 |
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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]. |
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| Related Catalog | |
| 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 |
| Molecular Formula | C28H30N4O3 |
|---|---|
| Molecular Weight | 470.56 |