ms39

MS 39 is a highly effective, highly affinity and selective depressant of mutant epidermal growth factor receptor (EGFR) with high efficiency, high affinity and selectivity. MS 39, conjured by gefitinib to VHL ligand via a linker, effectively induced the degradation of mutant EGFR (DC50 values in HCC827(exon 19 del) and H3255 (L858R mutation) lung cancer cell lines were 5 nM and 3.3 nM, respectively). However, there was no significant effect in wild-type EGFR cell lines with concentrations up to 10 μM. MS 39 inhibited the proliferation of H3255 lung cancer cells in vitro and was bioavailable in mice after administration.

MS39N (compound 27) serves as the negative control for MS39, capable of binding to EGFR without causing its degradation.

BMS-394136 (BMS 394136) is a KV1.5 antagonist for the treatment of cardiovascular diseases such as arrhythmias and atrial fibrillation.

MS 39N is a negative control for MS 39. Binds EGFR without inducing degradation.