Drug intelligence / Profile preview

AZ10606120

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intraperitoneal, Subcutaneous (preclinical Animal Studies)
01

Overview

AZ10606120 is a **potent, selective, high-affinity antagonist of the P2X7 receptor**, with Kd values of 1.4 nM (human) and 19 nM (rat)[1][9][7]. It acts as a **negative allosteric modulator**, binding to a site that is distinct from but coupled to the ATP binding site on the P2X7 receptor. AZ10606120 has demonstrated **anti-tumor and anti-angiogenic activity** in various preclinical cancer models, including melanoma, pancreatic cancer, mesothelioma, mammary cancer, neuroblastoma, and glioblastoma, by inhibiting tumor growth, cell proliferation, migration, invasion, and associated angiogenesis[2][6][3]. AZ10606120 has also been explored in non-cancer contexts such as **sepsis** (with mixed effects on vascular injury and hyperpermeability)[5][8], and **graft-versus-host disease** models[4]. The compound is used **mainly in research settings**. It is handled as its dihydrochloride salt in most studies.

Other names
AZ10606120 dihydrochlorideAZ-10606120 dihydrochlorideAZ 10606120 dihydrochloride
02

Targets

P2RX7 (P2X purinoceptor 7)

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