RTC-5

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].

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

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 Concentration: 0 μM, 1 μM, 10 μM, 20 μM, 30 μM, 40 μM Incubation Time: 48 hours Result: Inhibited H1650 lung adenocarcinoma cell growth. Western Blot Analysis[1] Cell Line: H1650 lung adenocarcinoma cells Concentration: 20 μM, 40 μM Incubation Time: 24 hours Result: Decreased p-AKT, p-ERK expression.

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