DDC-01-163 

DDC-01-163 is a mutant-selective allosteric PROTAC-based EGFR degrader, with an IC₅₀ of 45 nM (Pink: EGFR ligand (HY-151048); Black: linker (HY-W008005); Blue: CRBN ligand (HY-14658))^[1].

DDC-01-163 (0-10 μM) dose-dependently inhibits proliferation of L858R/T790M EGFR mutant Ba/F3 cells while sparing wildtype EGFR-Ba/F3 cells^[1].
DDC-01-163 exhibits an IC₅₀/EC₅₀ of 96 nM for EGFR in L858R/T790M cells^[2].

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

942.05

C₄₉H₅₁N₉O₉S

2140806-84-2

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCCOCCOCCOCCN4CCN(CC4)C5=CC=C(C6=CC=C7C(C(N(C(C8=CC=CC=C8)C(NC9=NC=CS9)=O)C7)=O)=C6)C=N5)=CC=C3)=O)=O

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• [1]. Jaebong Jang, et al. Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations. Angew Chem Int Ed Engl. 2020 Aug 17;59(34):14481-14489.  [Content Brief]

  [2]. Surya Kant Tripathi, et al. Allosteric mutant-selective fourth-generation EGFR inhibitors as an efficient combination therapeutic in the treatment of non-small cell lung carcinoma. Drug Discov Today. 2021 Jun;26(6):1466-1472.  [Content Brief]