PROTAC EGFR degrader 7 

PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR^L858R/T790M degrader, with a DC₅₀ of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC₅₀ of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research^[1]. PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

PROTAC EGFR degrader 7 (compound 13b) (BALB/c mice bearing NCI–H1975 cells, 10 mg/kg, IP, once a day for 24 days) effectively and selectively inhibits NCI–H1975 xenograft tumor growth, with the tumor growth inhibition (TGI%) of 63.7%^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

836.94

C₄₆H₄₈N₁₀O₆

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhang W, et al. Discovery of highly potent and selective CRBN-recruiting EGFRL858R/T790M degraders in vivo. Eur J Med Chem. 2022 Aug 5;238:114509.  [Content Brief]