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A2AR-antagonist-1

CAT: 0804-HY-149916Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-149916Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM) . A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min) . A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) [1].
CAS Number
2922920-71-4
UNSPSC
12352005
Target
Adenosine Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/a2ar-antagonist-1.html
Solubility
10 mM in DMSO
Smiles
O=C(N(CC1=CC=CC(C(O)(C)C)=C1)C=C2)C=C2C3=NC(N)=NC(C4=C(C)C(C#N)=CC=C4)=C3
Molecular Formula
C27H25N5O2
Molecular Weight
451.52
References & Citations
[1]Zhu C, et al. Discovery of Pyridinone Derivatives as Potent, Selective, and Orally Bioavailable Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2023 Mar 23.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Adenosine A2A receptor (A2AR)

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