Drug intelligence / Profile preview

CW-10201

Development stage
Unknown
Lead developer
University of Michigan
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01

Overview

CW-10201: sourced facts only. name: "CW-10201 effectively induced degradation of KRASG12D and KRASG12V mutants at low nanomolar concentrations in cells and attained IC50 values of 2-4 nM in inhibition of cell growth in cancer cell lines carrying KRASG12D or KRASG12V mutation." [PMID:42720481]; target: "CW-10201 effectively induced degradation of KRASG12D and KRASG12V mutants at low nanomolar concentrations in cells and attained IC50 values of 2-4 nM in inhibition of cell growth in cancer cell lines carrying KRASG12D or KRASG12V mutation." [PMID:42720481]; developer: "Department of Internal Medicine, University of Michigan, Ann Arbor, Michigan48109, United States." [PMID:42720481]; modality: "Herein, we present the design, synthesis, and evaluation of PROTAC KRAS degraders using a novel cereblon ligand, which led to the discovery of CW-10201 as a promising KRAS degrader." [PMID:42720481]; stage: "CW-10201 was capable of attaining tumor regression in the SW1990 KRASG12D mutated xenograft tumor model and effectively inhibited tumor growth in the SW620 KRASG12V xenograft tumor model in mice at well-tolerated doses." [PMID:42720481]

02

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