EGFR/C797S-IN-1 是一种有效的EGFR-C797S抑制剂，IC50值为 0.128 μM。EGFR/C797S-IN-1 显示出抗增殖活性和抗肿瘤活性。EGFR/C797S-IN-1 以剂量依赖的方式抑制 P-EGFR 蛋白的表达。
| 生物活性 | EGFR/C797S-IN-1 is a potentEGFR-C797Sinhibitor with anIC50value 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) |
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体外研究
(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. |
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体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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