eALM1137 is a highly potent, selective mTOR inhibitor with IC50 of 4.8 nM, weakly inhibits DNA-PK with IC50 of 77 nM (17-fold selectivity).
eALM1137 shows antiproliferative activity against GBM cell lines: U87-MG and T98G with IC50 of 5.1 nM and 11 nM.
eALM1137 does not inhibit PI3Kα, PKN3, CK1δ.
eALM1137 demonstrates dose-dependent dual inhibition of mTORC1 and mTORC2 activities, as shown by the reduction of S6 and Akt phosphorylation, respectively, at 30 nM and higher concentrations, in T98G and U87-MG cells.
eALM1137 treatment induces significant reduction in cell proliferation with an EC50 of 85 nM in triple mutant NPE cell line, which has a double deletion of NF1 and PTEN, and overexpression of EGFR in neural stem cells.
eALM1137 inhibits mTORC1 signaling, as evidenced by reduced phosphorylation of the S6 ribosomal protein (Ser235/236 and Ser240/244) and 4E-BP1 (Thr37/46).
