GLPBio

CPI-444 (V81444)

Catalog No.: GC32734Purity:>98.00%Synonyms: Ciforadenant
COASDSData Sheet
CPI-444 (V81444) (V81444) es un antagonista potente, activo por vÍa oral y selectivo del receptor de adenosina A2A (A2AR), que induce respuestas antitumorales.

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CPI-444 (V81444)
Cas No.: 1202402-40-1
10mM (in 1mL DMSO)In Stock
$53.00
1
5mgIn Stock
$48.00
1
10mgIn Stock
$77.00
1
25mgIn Stock
$148.00
1
50mgIn Stock
$221.00
1
100mgIn Stock
$315.00
1
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    610, 366–372 (2022)
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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Descripción (Description)

CPI-444 (V81444) is an orally available A2AAR antagonist with a Ki value of 3.54nM[1]. CPI-444 blocks the induction of cAMP by 1.5nM 5′-(N-Ethylcarboxamido) adenosine (NECA) with an IC50 value of 17.03nM[2]. CPI-444 inhibits the adenosine methionine (ADO) signaling pathway by antagonizing the A2AAR in the tumor microenvironment, stimulating the immune response mediated by T cells, thereby leading to tumor regression[3]. CPI-444 has been widely used to restrain tumor growth and metastasis, and to enhance oncolytic immunotherapy in animal models[4].

In vitro, CPI-444 treatment (10µM) for 1 hour significantly inhibited the suppressive effect of NECA on IFN-γ and IL-2 release from human peripheral blood mononuclear cells (hPBMCs)[2].

In vivo, daily oral administration of CPI-444 at a dose of 10mg/kg for 5 consecutive days enhanced the immune response to vaccinia-OVA and strengthened the memory response to viral infection in mice[5].

References:
[1] Zhang J, Yan W, Duan W, et al. Tumor immunotherapy using A2A adenosine receptor antagonists[J]. Pharmaceuticals, 2020, 13(9): 237.
[2] Willingham S B, Ho P Y, Hotson A, et al. A2AR antagonism with CPI-444 induces antitumor responses and augments efficacy to anti-PD-(L) 1 and anti-CTLA-4 in preclinical models[J]. Cancer immunology research, 2018, 6(10): 1136-1149.
[3] Deb P K, Maity P, Sarkar B, et al. Insights from clinical trials on A2A adenosine receptor antagonists for cancer treatment[J]. ACS Pharmacology & Translational Science, 2025, 8(6): 1498.
[4] Wu Y, Lin J Y, Zhou Y D, et al. Oncolytic peptide‐nanoplatform drives oncoimmune response and reverses adenosine‐induced immunosuppressive tumor microenvironment[J]. Advanced Healthcare Materials, 2024, 13(26): 2303445.
[5] Leone R D, Sun I M, Oh M H, et al. Inhibition of the adenosine A2a receptor modulates expression of T cell coinhibitory receptors and improves effector function for enhanced checkpoint blockade and ACT in murine cancer models[J]. Cancer immunology, immunotherapy, 2018, 67(8): 1271-1284.

Protocolo (Protocol)

Cell experiment [1]:

Cell lines

 Human peripheral blood mononuclear cells (hPBMCs)

Preparation Method

 hPBMCs were cultured in DMEM medium, supplemented with 10% fetal bovine serum, 1% penicillin-streptomycin, at 37°C in an incubator with 5% CO2. A total of 5×105 cells were incubated with 0.1μM NECA and different concentrations of CPI-444 (0, 0.1, 1, and 10µM) in a 96-well plate for 1 hour. Forty-eight hours later, levels of IFN-γ and IL-2 were analyzed.

Reaction Conditions

 0, 0.1, 1, and 10µM; 1h

Applications

 CPI-444 treatment markedly restored IL-2 and IFN-γ secretion in NECA-treated hPBMCs in a dose-dependent manner.
Animal experiment [2]:

Animal models

 C57BL/6 mice

Preparation Method

C57BL/6 mice (8 weeks old) were housed in specific pathogen-free conditions and fed standard mouse chow and water ad libitum. Mice were injected with 5×105 MC38 cells (s.c.) cultured in DMEM-based media. Mice were treated with CPI-444 (100mg/kg/day) or vehicle by gavage daily for 21 days and concentrations administered in 200µl volume. Tumor burden was assessed every 2-4 days by measuring length and width of tumor.

Dosage form

100mg/kg/day; 21 days; p.o.

Applications

CPI-444 treatment suppressed tumor burden in mice with MC38 xenografts.
References:
[1] Willingham S B, Ho P Y, Hotson A, et al. A2AR antagonism with CPI-444 induces antitumor responses and augments efficacy to anti-PD-(L) 1 and anti-CTLA-4 in preclinical models[J]. Cancer immunology research, 2018, 6(10): 1136-1149.
[2] Leone R D, Sun I M, Oh M H, et al. Inhibition of the adenosine A2a receptor modulates expression of T cell coinhibitory receptors and improves effector function for enhanced checkpoint blockade and ACT in murine cancer models[J]. Cancer immunology, immunotherapy, 2018, 67(8): 1271-1284.

Documentos del producto (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
1202402-40-1
Sinónimos
Ciforadenant
SMILES
NC1=NC(C2=CC=C(C)O2)=C(N=NN3CC4=NC(CO[C@@H]5COCC5)=CC=C4)C3=N1
Fórmula molecular
C20H21N7O3
Peso molecular
407.43
Solubilidad
DMSO : 67.5 mg/mL (165.67 mM)
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

Reviews

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