CI 988

Modify Date: 2024-01-02 10:27:33

CI 988 structure	Common Name	CI 988
	CAS Number	130332-27-3	Molecular Weight	614.73100
	Density	1.32g/cm3	Boiling Point	949.6ºC at 760mmHg
	Molecular Formula	C₃₅H₄₂N₄O₆	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of 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].

Name	4-[[(1R)-2-[[(2R)-2-(2-adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid
Synonym	More Synonyms

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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> Cholecystokinin Receptor Research Areas >> Neurological Disease
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].
In Vivo	CI-988 (10 mg/kg; p.o.; daily; for 20 days) inhibits the growth of colorectal cancer in xenografts model mice[3]. 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%.
References	[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.

Density	1.32g/cm3
Boiling Point	949.6ºC at 760mmHg
Molecular Formula	C₃₅H₄₂N₄O₆
Molecular Weight	614.73100
Exact Mass	614.31000
PSA	149.62000
LogP	6.03120
Vapour Pressure	0mmHg at 25°C
Index of Refraction	1.647

Precursor 10
CAS#:700-57-2 2-Adamantanol CAS#:56613-80-0 D-Plenylglycinol CAS#:53120-53-9 2-adamantyl chl... CAS#:130406-63-2 tricyclo[3.3.1....
CAS#:130406-35-8 Benzyl [(1R)-2-... CAS#:120666-53-7 Benzyl [(2R)-2-... CAS#:130406-38-1 N-[(benzyloxy)c... CAS#:130406-40-5 N-[(2-adamantyl...
CAS#:130406-37-0 toluene-4-sulfo... CAS#:130406-39-2 N-[(2-adamantyl...
DownStream 0