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CPI-444

Catalog No. T7183 CAS 1202402-40-1

Synonyms: V81444, ciforadenant

CPI-444 (V81444) is an antagonist of the adenosine A2A receptor.It reduces tumor area in mouse model of murine Her2/neu-expressing breast cancer.

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CPI-444, CAS 1202402-40-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 222.00
50 mg	In stock	$ 372.00
100 mg	In stock	$ 556.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 98%

Biological Description

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Description

CPI-444 (V81444) is an antagonist of the adenosine A2A receptor.It reduces tumor area in mouse model of murine Her2/neu-expressing breast cancer.

In vivo

CPI-444 is a potent, oral, selective A2AR antagonist that has been well tolerated in Ph 1/1b studies in non-oncology indications.?CPI-444 is being investigated in a Ph 1b study in solid tumors as a single agent and in combination with the anti-PD-L1 antibody atezolizumab.?In preclinical studies, daily treatment of the syngeneic mouse model MC38 with CPI-444 (1, 10, 100 mg/kg) led to dose-dependent inhibition of tumor growth, leading to tumor elimination in ～30% of treated mice.?Combining CPI-444 (100 mg/kg, qd, 14 days) with anti-PD-L1 (200 μg, 3qw, 4 doses) treatment in MC38 models synergistically inhibited tumor growth and eliminated tumors in 90% of treated mice.?When cured mice were later re-challenged with MC38 cells, tumor growth was rejected in 100% of challenged mice, indicating that CPI-444 induced systemic anti-tumor immune memory.?CD8+ T cell depletion abrogated 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 was 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[1].

Synonyms	V81444, ciforadenant
Molecular Weight	407.43
Formula	C20H21N7O3
CAS No.	1202402-40-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 67.5 mg/mL (165.67 mM)

References and Literature

1. Stephen Willingham, et al. Abstract PR04: CPI-444: A potent and selective inhibitor of A2AR induces antitumor responses alone and in combination with anti-PD-L1 in preclinical and clinical studies.Cancer Immunoly Research. September 25-28, 2016. 2. Willingham Stephen B, Ho Po Y, Hotson Andrew, et al. A2AR Antagonism with CPI-444 Induces Anti-Tumor Responses and Augments Efficacy to Anti-PD-(L)1 and Anti-CTLA-4 in Preclinical Models.[J]. Cancer Immunology Research:canimm.0056.2018-.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Neurodegenerative Disease Compound Library GPCR Compound Library Bioactive Compound Library Clinical Compound Library NO PAINS Compound Library

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Keywords

CPI-444 1202402-40-1 GPCR/G Protein Neuroscience Adenosine Receptor P1 receptor CPI444 Inhibitor V81444 CPI 444 V-81444 ciforadenant V 81444 inhibit inhibitor

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