MS 39 is a potent, high affinity and selective Degrader (PROTAC?) of mutant epidermal growth factor receptor (EGFR), comprising gefitinib(Iressa) conjugated via a linker to a VHL ligand. MS 39 potently induces degradation of mutant EGFR (DC50 values are 5 nM and 3.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) lung cancer cell lines, respectively), but exhibits no significant effect in cell lines bearing wild-type EGFR at concentrations up to 10 μM. MS 39 inhibits proliferation of H3255 lung cancer cellsin vitro, and is bioavailable in mice following ip administration.

MS 39 is a potent, high affinity and selective Degrader (PROTAC(R)) of mutant epidermal growth factor receptor (EGFR), comprising gefitinib(Iressa) conjugated via a linker to a VHL ligand. MS 39 potently induces degradation of mutant EGFR (DC50 values are 5 nM and 3.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) lung cancer cell lines, respectively), but exhibits no significant effect in cell lines bearing wild-type EGFR at concentrations up to 10 μM. MS 39 inhibits proliferation of H3255 lung cancer cellsin vitro, and is bioavailable in mice following ip administration.

MS 39

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years