Drug intelligence / Profile preview

cz415

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

CZ415 is a highly efficient and specific small molecule inhibitor of the mammalian target of rapamycin (mTOR) kinase, acting on both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2). It disrupts mTOR-mediated signaling by inhibiting the association of mTORC1 (mTOR-Raptor) and mTORC2 (mTOR-Rictor-GβL), resulting in reduced phosphorylation of mTORC1 substrates (S6K1, 4E-BP1) and mTORC2 substrate AKT. CZ415 induces apoptosis, cell cycle arrest, and autophagy, leading to reduced cell survival and proliferation in several cancer types including papillary thyroid carcinoma, head and neck squamous cell carcinoma, cervical cancer, and osteosarcoma. It shows tumor-suppressing effects both in vitro and in vivo in multiple animal tumor models[1][2][3][5][6].

02

Targets

mTOR (Mammalian target of rapamycin kinase)

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