CI-988

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].

Product Specifications

CAS Number

[130332-27-3]

Product Name Alternative

PD134308

UNSPSC

12352005

Target

Cholecystokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/ci-988.html

Solubility

10 mM in DMSO

Smiles

OC(CCC(N[C@H](C1=CC=CC=C1)CNC([C@](CC2=CNC3=C2C=CC=C3)(C)NC(OC4[C@H]5C[C@H](C6)C[C@@H]4C[C@H]6C5)=O)=O)=O)=O

Molecular Formula

C35H42N4O6

Molecular Weight

614.73

References & Citations

[1]Terry W Moody, et al. CI-988 Inhibits EGFR Transactivation and Proliferation Caused by Addition of CCK/Gastrin to Lung Cancer Cells. J Mol Neurosci. 2015 Jul;56 (3) :663-72.|[2]J Hughes, et al. Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc Natl Acad Sci U S A. 1990 Sep;87 (17) :6728-32.|[3]R Romani, et al. Gastrin receptor antagonist CI-988 inhibits growth of human colon cancer in vivo and in vitro. Aust N Z J Surg. 1996 Apr;66 (4) :235-7.