country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-191407

Copy Link Print Information

A2AR/A2BR antagonist 3

A2AR/A2BR antagonist 3 is a dual hA2A/hA2B adenosine receptor antagonist with K_i values of 9.0 nM and 11.4 nM, respectively. A2AR/A2BR antagonist 3 occupies the orthosteric pocket and antagonizes adenosine-driven Gs/cAMP signaling at both receptors, inhibiting CREB and ERK phosphorylation. A2AR/A2BR antagonist 3 restores T helper cytokine production and increases infiltration of cytotoxic T cells and helper T cells into tumors. A2AR/A2BR antagonist 3 can be used for research on colorectal cancer.

For research use only. We do not sell to patients.

CAS No.: 3146181-24-7
Formula: C₁₈H₂₂IN₇O₂
Molecular Weight:495.32

Storage:

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

Data Sheet (283 KB)

A2AR/A2BR antagonist 3 Chemical Structure

CAS No.: 3146181-24-7

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

hA_2AAR

9 nM (Ki)

hA_2B

11.4 nM (Ki)

All Adenosine Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Hep 3B2	GI50	46.0 μM	Inhibition of viability in human HEP3B cells after 72 hrs exposure to 5p by sulforhodamine B staining. Inhibition of viability in human HEP3B cells after 72 hrs exposure to 5p by sulforhodamine B staining.	acs.jmedchem.6c02638
CT26	GI50	23.1 μM	Inhibition of viability in mouse CT-26 cells after 72 hrs exposure to 5p by sulforhodamine B staining. Inhibition of viability in mouse CT-26 cells after 72 hrs exposure to 5p by sulforhodamine B staining.	acs.jmedchem.6c02638
SW48	GI50	35.8 μM	Inhibition of viability in human SW48 colorectal cells after 72 hrs exposure to 5p by sulforhodamine B staining. Inhibition of viability in human SW48 colorectal cells after 72 hrs exposure to 5p by sulforhodamine B staining.	acs.jmedchem.6c02638
MOLT-4	GI50	15.1 μM	Inhibition of viability in human MOLT4 hematologic cells after exposure to 5p by Calcein AM staining using 1 μM Calcein AM for 15 min at room temperature. Inhibition of viability in human MOLT4 hematologic cells after exposure to 5p by Calcein AM staining using 1 μM Calcein AM for 15 min at room temperature.	acs.jmedchem.6c02638
Jurkat	GI50	20.6 μM	Inhibition of viability in human Jurkat hematologic cells after exposure to 5p by Calcein AM staining using 1 μM Calcein AM for 15 min at room temperature. Inhibition of viability in human Jurkat hematologic cells after exposure to 5p by Calcein AM staining using 1 μM Calcein AM for 15 min at room temperature.	acs.jmedchem.6c02638

In Vitro

Anti-cancerOthers

Anti-cancer

A2AR/A2BR antagonist 3 (compound 5p) (1-10 µM; 1 h) inhibits NECA (5'-N-Ethylcarboxamidoadenosine) (HY-103173)-induced CREB phosphorylation in MOLT4 cells, with the greatest reduction at 5 µM across the tested dose series^[1].
A2AR/A2BR antagonist 3 (20 µM; 1 h) inhibits NECA-induced phosphorylation of CREB and ERK in SW48 cells^[1].
A2AR/A2BR antagonist 3 (20 µM; 1 h) reduces NECA-induced VEGFA mRNA expression in SW48 cells^[1].
A2AR/A2BR antagonist 3 inhibits the cell viability of Hepa1-6, HEP3B, CT-26, SW48, MOLT4, and Jurkat cells, with GI₅₀ values ranging from 15.1 to 46.0 µM^[1].

Others

A2AR/A2BR antagonist 3 (10 µM) is a potent dual hA2A/hA2B adenosine receptor binder, with Ki values of 9.0 nM and 11.4 nM for hA2A and hA2B, respectively^[1].
A2AR/A2BR antagonist 3 (10 µM; 1 h) antagonizes NECA-induced cAMP accumulation in cells expressing hA2A and hA2B, with IC₅₀ values of 0.38 µM and 0.05 µM, respectively^[1].

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

Western Blot Analysis^[1]

Cell Line:

MOLT4 cells
Concentration:

1, 2, 5 ,10 µM
Incubation Time:

1 h
Result:

Inhibited NECA-induced CREB phosphorylation.

Western Blot Analysis^[1]

Cell Line:

SW48 cells
Concentration:

20 µM
Incubation Time:

1 h
Result:

Inhibited NECA-induced phosphorylation of CREB and ERK in SW48 cells.

RT-PCR^[1]

Cell Line:

SW48 cells
Concentration:

20 µM
Incubation Time:

1 h
Result:

Suppressed NECA-induced VEGFA mRNA expression.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_0-t	AUC_0-∞	T_1/2
Mice^[1]	10 mg/kg	i.p.	0.25 h	3857 ng/mL	6249 ng·h/mL	6269 ng·h/mL	0.82 h

In Vivo

Anti-cancerAdaptive Immunity

Anti-cancer

A2AR/A2BR antagonist 3 (compound 5p) (100 mg/kg for the first three days, followed by 75 mg/kg daily until day 17; i.p.; daily) inhibits tumor growth in the CT26 subcutaneous colorectal cancer model^[1].

Anti-cancer

Adaptive Immunity

A2AR/A2BR antagonist 3 (100 mg/kg for the first three days, followed by 75 mg/kg daily up to day 17; i.p.; daily) more strongly inhibits tumor growth in CT26-CD73^hi tumors and increases CD8⁺ and CD4⁺ T cell infiltration^[1].

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

Animal Model:

BALB/c (female, 6 weeks old)^[1]
Dosage:

100 mg/kg for the first three days, followed by 75 mg/kg daily up to day 17
Administration:

i.p.; daily
Result:

Inhibited tumor growth in a CT26 subcutaneous colorectal cancer model.
Tumor growth was more strongly inhibited in CT26-CD73^hi tumors, with increased infiltration of CD8+ and CD4+ T cells.

Related Protocols :

Chemical Information

CAS No. 3146181-24-7
Molecular Weight 495.32
Formula C₁₈H₂₂IN₇O₂
SMILES

O=C(NCCN1CCN(C)CC1)NC2=CN3C(C(C4=CC=CO4)=N2)=NC=C3I
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Kim C, et al. Imidazo[1,2-a]pyrazine Derivatives as Dual A₂A/A₂B Adenosine Receptor Antagonists Enhancing Anti-PD-1 Antibody Therapy in Colorectal Cancer. J Med Chem.

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote

Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

A2AR/A2BR antagonist 3

All Adenosine Receptor Isoforms

Biological Activity

Description

IC50 & Target

Cellular Effect

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs