RTC-5

RTC-5 是一种具有抗癌效力的优化吩噻嗪。RTC-5 显示针对 EGFR 驱动的癌症的异种移植模型的功效，其效果归因于 PI3K-AKT 和 RAS-ERK 信号传导的负调节。

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Background

RTC-5 is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling[1]. IC50: EGFR[1]

RTC-5 (0-40 μM; 48 hours) inhibits H1650 lung adenocarcinoma cell growth with an GI50 of 12.6μM[1].RTC-5 (20-40 μM; 24 hours) negatively regulates PI3K-AKT and RAS-ERK pathways by decreasing phospho-AKT and phospho-ERK levels expression[1]. Cell Viability Assay[1] Cell Line: H1650 lung adenocarcinoma cells

[1]. Kastrinsky DB, et al. Reengineered tricyclic anti-cancer agents. Bioorg Med Chem. 2015 Oct 1;23(19):6528-34.