Drug intelligence / Profile preview

9c

Development stage
Preclinical
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Oral
01

Overview

9c is an HSP90-mediated targeting chimera (HEMTAC) based WEE1-target degrader. It is designed to enhance efficiency and decrease off-tumor risks associated with targeted protein degradation technologies. 9c effectively degrades cellular WEE1 protein, leading to superior anti-proliferative activity in MV-4-11 cells by inducing cell cycle arrest in the G2/M phase. It demonstrates high selectivity for primary acute myeloid leukemia (AML) cells over normal cells and has shown superior anti-cancer activity and lower hematotoxicity compared to AZD1775 in an AML PDX model. 9c is being developed as a promising degrader for AML target therapy.

02

Targets

HSP90 (Heat shock protein 90 chaperone complex)WEE1 (WEE1 G2 checkpoint kinase)

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