CI-988 (PD134308) is a potent, selective and orally activeCCK2R (cholecystokinin 2 receptor)antagonist with anIC₅₀of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects^[1][2][3].

IC50: 1.7 nM (Mouse cortex CCK2); 2717 nM (Rat pancreas CCK1)^[2]

CI-988 inhibits specific¹²⁵I-BH-CCK-8 binding to NCI-H727 cells with high affinity (K_iof 4.5 nM). The increase in ROS caused by CCK-8 addition to NCI-727 cells is blocked significantly by CI-988. CI-988 (3 μM) inhibits the basal growth of NCI-H727 cells or that stimulated by CCK-8. CI-988 inhibits the ability of CCK-8 to cause ERK phosphorylation and elevate cytosolic Ca^2+[1].
CI-988 inhibits in a dose-dependent manner the ability of CCK-8 to cause EGFR transactivation in NCI-H727 cells. CI-988 at doses of 1 and 10 μM weakly and strongly, respectively, inhibits the ability of 0.1μM CCK-8 to increase EGFR tyrosine phosphorylation. CI-988 antagonizes the ability of CCK-8 to cause lung cancer EGFR or ERK tyrosine phosphorylation^[1].

CI-988 (10 mg/kg; p.o.; daily; for 20 days) inhibits the growth of colorectal cancer in xenografts model mice^[3].

614.73

C₃₅H₄₂N₄O₆

130332-27-3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.