Taminadenant

Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972) . Taminadenant reactivate the antitumor immune response[1][2].

Product Specifications

CAS Number

[1337962-47-6]

Product Name Alternative

NIR178; PBF509

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Adenosine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Taminadenant.html

Purity

99.84

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

BrC(C(N1C=CC=N1)=NC(N2C=CC=N2)=N3)=C3N

Molecular Formula

C10H8BrN7

Molecular Weight

306.12

Precautions

H302, H315, H319, H335

References & Citations

[1]Núñez F, et al. PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders. Front Pharmacol. 2018 Oct 19;9:1200.|[2]Chiappori AA, et al. Phase I Study of Taminadenant (PBF509/NIR178), an Adenosine 2A Receptor Antagonist, with or without Spartalizumab (PDR001), in Patients with Advanced Non-Small Cell Lung Cancer. Clin Cancer Res. 2022 Jun 1;28 (11) :2313-2320.