2. GPCR/G Protein
  3. Adenosine Receptor
  4. INCB106385

INCB106385 is an orally active A2A/A2B adenosine receptor antagonist, with an IC50 value of 4.4 nM for cAMP inhibition at the A2A adenosine receptor and an IC50 value of 6.4 nM for cAMP inhibition at the A2B adenosine receptor. INCB106385 inhibits the pCREB signaling pathway in immune cells, blocks adenosine-mediated immunosuppression in the tumor microenvironment, and induces tumor regression. INCB106385 exhibits efficacy as a monotherapy or in combination with anti-PD-1 antibodies in colon cancer models. INCB106385 can be used for the research of colon cancer.

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INCB106385

INCB106385 Chemical Structure

CAS No. : 2408260-34-2

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INCB106385 Related Antibodies

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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Description

INCB106385 is an orally active A2A/A2B adenosine receptor antagonist, with an IC50 value of 4.4 nM for cAMP inhibition at the A2A adenosine receptor and an IC50 value of 6.4 nM for cAMP inhibition at the A2B adenosine receptor. INCB106385 inhibits the pCREB signaling pathway in immune cells, blocks adenosine-mediated immunosuppression in the tumor microenvironment, and induces tumor regression. INCB106385 exhibits efficacy as a monotherapy or in combination with anti-PD-1 antibodies in colon cancer models. INCB106385 can be used for the research of colon cancer[1].

IC50 & Target[1]

A2AR

 

A2BR

 

In Vitro

INCB106385 (compound 36) inhibits cAMP production in A2A-overexpressing HEK293 cells with an IC50 of 4.4 nM[1].
INCB106385 inhibits cAMP production in A2B-overexpressing HEK293 cells with an IC50 of 6.4 nM[1].
INCB106385 inhibits phospho-CREB levels in human whole blood CD4+ T cells with an IC50 of 4.1 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

INCB106385 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Cmax AUC Bioavailability
Rat[1] 1.0 mg/kg i.v. 8.7 h / 27300 nM·h /
Rat[1] 3.0 mg/kg p.o. / 18200 nM 27300 nM·h 108 %
Cynomolgus Monkey[1] 1.0 mg/kg i.v. 5.8 h / / /
Cynomolgus Monkey[1] 3.0 mg/kg p.o. / 3870 nM 12500 nM·h 80 %
Molecular Weight

435.44

Formula

C23H17N9O
CAS No.
SMILES

N#CC1=CC=CC(C2=C(C(C=C3)=NN(C)C3=O)N4C(C(N)=N2)=NC(CC5=NC=CC=C5)=N4)=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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INCB106385 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

INCB1063852408260-34-2INCB 106385INCB-106385Adenosine ReceptorP1 receptorA2B adenosine receptoranti-PD-1 antibodyCD4+ T cellscolon carcinomaHEK293 cellsimmune cellsA1 adenosine receptorpCREB signalingtumor microenvironment immune suppressionA2A adenosine receptorInhibitorinhibitorinhibit

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