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D16-M1P2

Development stage
Preclinical
Lead developer
InSilico Medicine
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

D16-M1P2 is a first-in-class proteolysis-targeting chimera (PROTAC) developed by Insilico Medicine using their AI-driven Chemistry42 platform. It is designed to target Membrane-associated Tyrosine/Threonine Protein Kinase 1 (PKMYT1), a key regulator of the cell cycle. D16-M1P2 features a unique dual mechanism of action, simultaneously inducing the degradation of PKMYT1 through the ubiquitin-proteasome system and directly inhibiting its kinase activity. Preclinical studies have demonstrated that the compound is highly selective, shows potent anti-tumor activity in xenograft models, and possesses favorable oral bioavailability. D16-M1P2 is currently in the pre-candidate validation stage for the treatment of cancer, offering a more durable effect compared to traditional PKMYT1 inhibitors.

02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)RAF1 (c-Raf-1 (Y340D/Y341D))CRBN (Cereblon)PKMYT1 (Protein kinase membrane associated tyrosine/threonine 1)

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