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ChemicalBook >> CAS DataBase List >>CPI-444

CPI-444

CAS No.
1202402-40-1
Chemical Name:
CPI-444
Synonyms
V81444;CPI-444;CPD1110;CS-2828;Ciforadenant;CPI-444 AND7648;CPI-444 (V81444);CPI-444, Ciforadenant;CPI-444;CPI 444;CPI444;Ciforadenant (CPI-444)
CBNumber:
CB42663793
Molecular Formula:
C20H21N7O3
Molecular Weight:
407.43
MDL Number:
MFCD31540410
MOL File:
1202402-40-1.mol
Last updated:2023-09-20 16:43:00

CPI-444 Properties

Melting point 169-171°C
Boiling point 676.9±65.0 °C(Predicted)
Density 1.55±0.1 g/cm3(Predicted)
storage temp. -20°C
solubility Soluble in DMSO (up to at least 25 mg/ml)
form solid
pka 4.05±0.30(Predicted)
color Beige
Stability Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
FDA UNII 8KFO2187CP

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P280-P301+P312-P302+P352-P305+P351+P338
NFPA 704
0
2 0

CPI-444 price More Price(15)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 25024 CPI-444 ≥98% 1202402-40-1 1mg $44 2024-03-01 Buy
Cayman Chemical 25024 CPI-444 ≥98% 1202402-40-1 5mg $151 2024-03-01 Buy
Cayman Chemical 25024 CPI-444 ≥98% 1202402-40-1 10mg $278 2024-03-01 Buy
Cayman Chemical 25024 CPI-444 ≥98% 1202402-40-1 25mg $638 2024-03-01 Buy
TRC C781455 CPI-444 1202402-40-1 25mg $450 2021-12-16 Buy
Product number Packaging Price Buy
25024 1mg $44 Buy
25024 5mg $151 Buy
25024 10mg $278 Buy
25024 25mg $638 Buy
C781455 25mg $450 Buy

CPI-444 Chemical Properties,Uses,Production

Description

CPI-444 (1202402-40-1) is a potent (Ki = 3.54 nM) and selective adenosine A2A receptor antagonist. It blocked the induction of cAMP induced by NECA in HEK-293 cells with an IC50 = 17.03 nM. CPI-444 monotherapy or in combination with anti-PD-1, anti-PD-L1, and anti-CTLA-4 induced T-cell-mediated tumor responses, inhibited tumor growth, and enabled antitumor immune memory. Currently in clinical trials for multiple cancers.

Uses

CPI-444 is an orally administered antagonist to the A2A receptor, and binds to adenosine receptors on the surface of immune cells.

Biological Functions

CPI-444 is a small molecule, oral, checkpoint inhibitor designed to disable a tumor’s ability to subvert attack by the immune system by blocking the binding of adenosine in the tumor microenvironment to the A2A receptor. Adenosine, a metabolite of ATP (adenosine tri-phosphate), is produced within the tumor microenvironment where it may bind to the adenosine A2A receptor present on immune cells and block their activity. CD39 and CD73 are enzymes on the surface of tumor cells and immune cells. These enzymes work in concert to convert ATP to adenosine. In vitro and preclinical studies have shown that dual blockade of CD73 and the A2A receptor may be synergistic.

in vitro

CPI-444 is a potent, oral, selective A2AR antagonist. CD8+ T cell depletion abrogates the efficacy of CPI-444 treatment as a single agent as well as in combination with anti-PD-L1, demonstrating a role for CD8+ T cells in mediating primary and secondary immune responses. Anti-tumor efficacy of CPI-444±anti-PD-L1 is associated with increased CD8+ cell infiltration and activation in MC38 tumor tissues, and a corresponding rise in PD-1 expression on CD8+ T cells in the spleen. Additionally, levels of immune checkpoints are modulated by treatment with CPI-444, including GITR, OX40, and LAG3 on tumor infiltrating lymphocytes and circulating T cells, suggesting a broad role for adenosine mediated immunosuppression.

References

1) Willingham?et al.?(2018),?A2AR Antagonism with CPI-444 Induces Antitumor Responses and Augments Efficacy to Anti-PD-(L)1 and Anti-CTLA-4 in Preclinical Models;?Cancer Immunol. Res.?6?1136 2) Leone?et al.?(2018),?), 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;?Cancer Immunol. Immunother.?671271 3) NCT02655822

1202402-82-1
338998-93-9
1202402-40-1
Synthesis of CPI-444 from (S)-7-chloro-3-((6-(((tetrahydrofuran-3-yl)oxy)methyl)pyridin-2-yl)methyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine and 2-Methylfurane-5-boronic acid pinacol ester
Global( 96)Suppliers
Supplier Tel Email Country ProdList Advantage
Amadis Chemical Company Limited
571-89925085 sales@amadischem.com China 131957 58
Capot Chemical Co.,Ltd. 		+86-（0）57185586718 +86-13336195806 sales@capot.com China 29793 60
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32956 60
career henan chemical co 		+86-0371-86658258 +8613203830695 sales@coreychem.com China 29880 58
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HANGZHOU CLAP TECHNOLOGY CO.,LTD 		86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6312 58
ANHUI WITOP BIOTECH CO., LTD 		+8615255079626 eric@witopchemical.com China 23541 58
Finetech Industry Limited 		+86-27-87465837 +8618971612321 info@finetechnology-ind.com China 9639 58
Zhejiang J&C Biological Technology Co.,Limited 		+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10473 58
InvivoChem 		+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58

View Lastest Price from CPI-444 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
CPI-444 pictures 2022-01-14 CPI-444
1202402-40-1
 US $0.00 / KG 1KG 97.4% 100 tons Honest Joy Holdings Limited
(S)-7-(5-Methyl-furan-2-yl)-3-[6-(tetrahydro-furan-3-yloxyMethyl)-pyridin-2-ylMethyl]-3H-[1,2,3]triazolo[4,5-d]pyriMidin-5-ylaMine pictures 2019-09-02 (S)-7-(5-Methyl-furan-2-yl)-3-[6-(tetrahydro-furan-3-yloxyMethyl)-pyridin-2-ylMethyl]-3H-[1,2,3]triazolo[4,5-d]pyriMidin-5-ylaMine
1202402-40-1
 US $1.00 / KG 1KG 98% 1lg; 2kg; 5kg; 10kg; 100kg Career Henan Chemical Co
  • CPI-444 pictures
  • CPI-444
    1202402-40-1
  • US $0.00 / KG
  • 97.4%
  • Honest Joy Holdings Limited

CPI-444 Spectrum

1202402-40-1(CPI-444)Related Search:

(S)-7-(5-Methyl-furan-2-yl)-3-[6-(tetrahydro-furan-3-yloxyMethyl)-pyridin-2-ylMethyl]-3H-[1,2,3]triazolo[4,5-d]pyriMidin-5-ylaMine CPD1110 CPI-444 7-(5-Methyl-2-furanyl)-3-[[6-[[[(3S)-tetrahydro-3-furanyl]oxy]methyl]-2-pyridinyl]methyl]-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-amine Triazolo-pyramidine derivative 3H-1,2,3-Triazolo[4,5-d]pyrimidin-5-amine, 7-(5-methyl-2-furanyl)-3-[[6-[[[(3S)-tetrahydro-3-furanyl]oxy]methyl]-2-pyridinyl]methyl]- CPI-444 AND7648 (S)-5-Amino-7-(5-methyl-2-furyl)-3-[[6-[[(3-tetrahydrofuranyl)oxy]methyl]-2-pyridyl]methyl]-3H-[1,2,3]triazolo[4,5-d]pyrimidine Ciforadenant (CPI-444) CPI-444;CPI 444;CPI444 (S)-7-(5-Methylfuran-2-yl)-3-((6-(((tetrahydrofuran-3-yl)oxy)methyl)pyridin-2-yl)methyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine CS-2828 Ciforadenant CPI-444 (V81444) V81444 (S)-3-{6-[(tetrahydrofuran-3-yloxy)methyl]pyridin-2-ylmethyl}-7-(5-methyl-2-furyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-ylamine 7-(5-methylfuran-2-yl)-3-[(6-{[(3S)-oxolan-3-yloxy]methyl}pyridin-2-yl)methyl]-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine CPI-444, Ciforadenant 1202402-40-1 APIs