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Table 1 In vitro activity of DZD2269 on four adenosine receptors

From: Overcoming high level adenosine-mediated immunosuppression by DZD2269, a potent and selective A2aR antagonist

  

Adenosine

NECA

 

Conc. (µM)

10

100

1

10

IC50 (nM)

A2aR

0.96 ± 0.36

(n = 23)

24 ± 4.6

(n = 6)

2.1 ± 0.39

(n = 6)

28 ± 4.2

(n = 6)

A2bR

106 ± 16

(n = 8)

2042 ± 267

(n = 6)

217 ± 47

(n = 6)

2276 ± 388

(n = 6)

A1R

8431 ± 1100

(n = 23)

> 10,000

(n = 6)

3235 ± 741

(n = 6)

> 10,000

(n = 6)

A3R

> 10,000

(n = 8)

> 10,000

(n = 6)

> 10,000

(n = 6)

> 10,000

(n = 6)

  1. Cells were stimulated with different concentrations of Adenosine or 5’-N-ethylcarboxamide adenosine (NECA). cAMP was used as a readout for CHO-A2aR and CHO-A2bR, intracellular calcium was used as a readout for CHO-A1R and CHO-A3R cells. Values are expressed as average ± SD of independent experiments