Your company account is blocked and you cannot place orders. If you have questions, please contact your company administrator.

Ciforadenant (CPI-444) - 99%, high purity , Adenosine A2a receptor antagonist, CAS No.1202402-40-1, Adenosine A2a receptor antagonist

Item Number
C413566
Grouped product items
SKUSizeAvailabilityPrice Qty
C413566-5mg
5mg
In stock
$98.90
C413566-25mg
25mg
In stock
$445.90
C413566-100mg
100mg
In stock
$741.90

Adenosine Receptor Antagonists

Basic Description

SynonymsNSC801812 | NSC-801812 | EX-A1716 | UNII-8KFO2187CP | HY-101978 | s6646 | ciforadenant | Ciforadenant [USAN:INN] | A-chloroethyl) phosphate | V81444;Triazolo-pyramidine derivative | CPI 444 | (S)-7-(5-methylfuran-2-yl)-3-((6-(((tetrahydrofuran-3-yl)oxy)me
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsCiforadenant\xa0(CPI-444, V81444) is a potent and selective Adenosine A2A receptor antagonist. It binds to A2A receptors with a Ki of 3.54 nmol/L and demonstrates a greater than 50-fold selectivity for the A2A receptor over other adenosine receptor subtyp
Storage TempStore at -20°C,Argon charged
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAdenosine A2a receptor antagonist
Product Description

Information

Ciforadenant (CPI-444) Ciforadenant (CPI-444, V81444) is a potent and selective Adenosine A2A receptor antagonist. It binds to A2A receptors with a Ki of 3.54 nmol/L and demonstrates a greater than 50-fold selectivity for the A2A receptor over other adenosine receptor subtypes.


Targets

A2AR 3.54 nM(Ki)


In vitro

CPI-444 restores T-cell activation in vitro.


In vivo

CPI-444 treatment resulted in a similar inhibition of tumor growth in the B16F10 melanoma (100 mg/kg) and RENCA renal cell cancer syngeneic models (10 mg/kg). It enhances T-cell activation in both the periphery and tumor microenvironment.

Product Properties

ALogP1.769
HBD Count1
Rotatable Bond6

Associated Targets(Human)

ADORA2A Tclin Adenosine receptor A2a (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ADORA1 Tclin Adenosine A1 receptor (17603 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA2A Tclin Adenosine A2a receptor (16305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA2B Tclin Adenosine A2b receptor (7672 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences
Adenosine A1 receptor partial agonistPARTIAL AGONISTALA226Adenosine A1 receptorSINGLE PROTEINHomo sapiens

PubMed: [1] , [2] , [3]


Adenosine A1 receptor agonistAGONISTALA226Adenosine A1 receptorSINGLE PROTEINHomo sapiens

PubMed: [1] , [2]


Adenosine A1 receptor antagonistANTAGONISTALA226Adenosine A1 receptorSINGLE PROTEINHomo sapiens

DOI: [1]


PubMed: [1]


Adenosine A1 receptor agonistAGONISTALA226Adenosine A1 receptorSINGLE PROTEINHomo sapiens

PubMed: [1]


Adenosine A1 receptor antagonistANTAGONISTALA226Adenosine A1 receptorSINGLE PROTEINHomo sapiens

PubMed: [1]


Adenosine A1 receptor agonistAGONISTALA226Adenosine A1 receptorSINGLE PROTEINHomo sapiens

PubMed: [1] , [2] , [3]


Adenosine A1 receptor agonistAGONISTALA226Adenosine A1 receptorSINGLE PROTEINHomo sapiens

Other: [1]


Adenosine A1 receptor antagonistANTAGONISTALA226Adenosine A1 receptorSINGLE PROTEINHomo sapiens

Other: [1]


Adenosine A1 receptor agonistAGONISTALA226Adenosine A1 receptorSINGLE PROTEINHomo sapiens
Adenosine A1 receptor agonistAGONISTALA226Adenosine A1 receptorSINGLE PROTEINHomo sapiens

Other: [1]


PubMed: [1]


Names and Identifiers

Pubchem Sid504770362
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/504770362
IUPAC Name 7-(5-methylfuran-2-yl)-3-[[6-[[(3S)-oxolan-3-yl]oxymethyl]pyridin-2-yl]methyl]triazolo[4,5-d]pyrimidin-5-amine
INCHI InChI=1S/C20H21N7O3/c1-12-5-6-16(30-12)17-18-19(24-20(21)23-17)27(26-25-18)9-13-3-2-4-14(22-13)10-29-15-7-8-28-11-15/h2-6,15H,7-11H2,1H3,(H2,21,23,24)/t15-/m0/s1
InChi Key KURQKNMKCGYWRJ-HNNXBMFYSA-N
Canonical SMILES CC1=CC=C(O1)C2=C3C(=NC(=N2)N)N(N=N3)CC4=NC(=CC=C4)COC5CCOC5
Isomeric SMILES CC1=CC=C(O1)C2=C3C(=NC(=N2)N)N(N=N3)CC4=NC(=CC=C4)CO[C@H]5CCOC5
PubChem CID 44537963
Molecular Weight 407.43

Certificates

C of A & Other Certificates

Find and download the COA for your product by matching the lot number on the packaging.

3 results found

Lot NumberCertificate TypeDateItem
J2213443Certificate of AnalysisJul 24, 2022 C413566
J2213485Certificate of AnalysisJul 24, 2022 C413566
J2213500Certificate of AnalysisJul 24, 2022 C413566

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 81 mg/mL (198.8 mM); Water: Insoluble; Ethanol: Insoluble;DMSO (Slightly), Methanol (Slightly)
DMSO(mg / mL) Max Solubility81
DMSO(mM) Max Solubility198.807157057654
Water(mg / mL) Max Solubility<1

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H335:May cause respiratory irritation

Precautionary Statements

P261:Avoid breathing dust/fume/gas/mist/vapors/spray.

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

Related Documents

References

1. Leone RD, Sun IM, Oh MH, Sun IH, Wen J, Englert J, Powell JD.  (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,  67  (8): (1271-1284).  [PMID:29923026] [10.1021/op500134e]
2. Willingham SB, Ho PY, Hotson A, Hill C, Piccione EC, Hsieh J, Liu L, Buggy JJ, McCaffery I, Miller RA.  (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,  (10): (1136-1149).  [PMID:30131376] [10.1021/op500134e]

Solution Calculators