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Cat. No.: HY-184213

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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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CAS No.: 2408260-34-2
Formule: C₂₃H₁₇N₉O
Masse moléculaire:435.44

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

INCB106385 Chemical Structure

CAS No.: 2408260-34-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

IC₅₀ & Target

^[1]

A2AR

A2BR

Voir tous les produits spécifiques à Isoform Adenosine Receptor :

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.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	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 %

Chemical Information

CAS No. 2408260-34-2
Masse moléculaire 435.44
Formule C₂₃H₁₇N₉O
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Qi C, et al. Discovery of Dual A2A/A2B Adenosine Receptor Antagonist and Clinical Candidate INCB106385. J Med Chem. 2026 Jun 11;69(11):13899-13918. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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