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Adenosine receptor antagonist 2

Names

[ CAS No. ]:
2703054-47-9

[ Name ]:
Adenosine receptor antagonist 2

Biological Activity

[Description]:

Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

[Target]

A2a adenosine receptor:1 nM (IC50)

A2b adenosine receptor:3 nM (IC50)


[In Vivo]

Adenosine receptor antagonist 2 (compound L-1; po; 10, 30, 100 mg/kg; twice a day for 22 days) inhibits tumor growth in female C57BL / 6mice mice with MC38(#22)-hpd-L1 cells[1]. Adenosine receptor antagonist 2 (iv; 2 mg/kg) has a CLz of 14.7 mL/min·kg and an AUC of 2252 h·ng/mL. Adenosine receptor antagonist 2 (po; 10 mg/kg) has a Cmax of 8730 ng/mL in adult male ICR mice (weight 25-40g)[1].

[References]

[1]. Lifeng Liu, et al. Substituted pyrimidine or Pyridylamine derivatives, their compositions and pharmaceutical uses. WO2021185256A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H21FN8O

[ Molecular Weight ]:
444.46


Related Compounds