BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK PTK6), displaying an IC50 of 30 nM. Additionally, it effectively suppresses p-SAM68 with an IC50 value of 52 nM. This compound, BRK inhibitor P21d hydrochloride, serves as a valuable tool for evaluating the efficacy of BRK inhibitors in xenograft breast tumor models, enabling the assessment of their in vivo activity.
EGFR-IN-52 (Compound 4) is a highly effective inhibitor of the epidermal growth factor receptor (EGFR). It exhibits IC50 values of 0.358, 86.02, and 432.67 μM against EGFR, EGFR L858R-TK, and EGFR T790M-TK, respectively. Additionally, EGFR-IN-52 demonstrates potent cytotoxic effects on cancer cell lines and triggers apoptosis [1].
CB1 2 agonist 3 (compound52), a potent non-selective cannabinoid ligand, is a competitive agonist for the CB1 CB2 receptors. It exhibits CB1 CB2 agonistic activity by binding to the human CB1 and CB2 receptors, with Ki values of 5.9 nM and 3.5 nM, respectively [1].