T-1-PMPA is a potent EGFR inhibitor with apoptotic properties. T-1-PMPA effectively inhibits EGFRWT and EGFR790m, with IC50 values of 86 nM and 561.73 nM, respectively.
T-1-PMPA (0.312-10 μM; 24 h) shows significant suppression of the proliferation of HepG2 and MCF7 malignant cell lines, with IC50 values of 3.51 μM and 4.13 μM, respectively[1]. In HepG2 cells, T-1-PMPA increases the proportion of cells in the early stage of apoptosis from 0.77 to 29.17%, the late stage of apoptosis from 0.17 to 8.81%, and the overall stage from 3.05 to 42.03%. Additionally, the percentage of necrotic cells increased to 4.05% compared to 2.21% in the control cells. The qRT-PCR analysis further supported the apoptotic effects by revealing significant increases in the levels of caspase-3 and caspase-9. T-1-PMPA controlls the levels of TNFα and IL2 by 74 and 50%[1].
References:
[1]. Ibrahim H Eissa, et al. New Theobromine Apoptotic Analogue with Anticancer Potential Targeting the EGFR Protein: Computational and In Vitro Studies. ACS Omega. 2024 Mar 27;9(14):15861-15881.