CPI-444

SKU: orb1300002

Description

CPI-444

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1202402-40-1
• MW: 407.43
• Purity: 98.78%
• Formula: C₂₀H₂₁N₇O₃
• SMILES: Cc1ccc(o1)-c1nc(N)nc2n(Cc3cccc(CO[C@H]4CCOC4)n3)nnc12
• Target: Adenosine Receptor
• Solubility: DMSO:67.5 mg/mL (165.67 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (6.14 mM)

Bioactivity

• 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.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

A2A, Adenosine Receptor, AdenosineReceptor, ciforadenant, CPI444, CPI-444, CPI 444, Inhibitor, inhibit, P1 receptor, V81444, V-81444, V 81444

Compound Identifiers

PubChem CID

44537963