1. GPCR/G Protein
    Neuronal Signaling
  2. Cholecystokinin Receptor
  3. CI-988

CI-988 (Synonyms: PD134308)

Cat. No.: HY-105226
Handling Instructions

CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 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.

For research use only. We do not sell to patients.

CI-988 Chemical Structure

CI-988 Chemical Structure

CAS No. : 130332-27-3

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Description

CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 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 & Target

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

In Vitro

CI-988 inhibits specific 125I-BH-CCK-8 binding to NCI-H727 cells with high affinity (Ki of 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 Ca2+[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice injected with LoVo cells[3]
Dosage: 10 mg/kg
Administration: p.o.; daily; for 20 days
Result: Inhibited the growth of xenografts by 53%.
Molecular Weight

614.73

Formula

C₃₅H₄₂N₄O₆

CAS No.
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CI-988
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HY-105226
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