DDC-01-163

DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772) -resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer[1].

Product Specifications

CAS Number

[2140806-84-2]

UNSPSC

12352005

Target

EGFR; PROTACs

Type

Reference compound

Related Pathways

JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ddc-01-163.html

Purity

99.05

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C49H51N9O9S

Molecular Weight

942.05

References & Citations

[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.|[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.|[3]Jang J, 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.