MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.
FC 11 is a highly potent focal adhesion Ki nase (FAK) PROTAC®Degrader (DC50 values are 40 to 370 pM depending on cell line), which is composed of the FAK inhibitor PF 562217 joined by a linker to the cereblon-binding ligand Pomalidomide. The effects of FC 11 are reversible upon compound wash out. FC 11 also degrades autophosphorylated FAK (pFAKtyr397), displaying near complete degradation after 3 hours at 100 nM in TM3 cells.
cIAP1 Ligand-Linker Conjugates 11 Hydrochloride is a chemical compound consisting of an IAP ligand that targets the E3 ubiquitin ligase, along with a PROTAC linker. It is primarily utilized in the development of SNIPERs, a molecular tool for targeted protein degradation[1].
cIAP1 Ligand-Linker Conjugates 11 is a chemical compound that combines an IAP ligand specifically designed for the E3 ubiquitin ligase with a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 11, is useful in the development of SNIPERs[1], allowing for the targeted degradation of proteins.
m-PEG11-acid is a non-cleavable 11-unit polyethylene glycol (PEG) linker utilized in the synthesis of antibody-drug conjugates (ADCs) [1]. It is similarly employed as a PEG-based linker for PROTAC synthesis [2].