CI-988 hemihydrate (Synonyms: PD134308 hemihydrate)

Cat. No.: HY-105226B: FAQs
Data Sheet Handling Instructions

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CI-988 hemihydrate (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 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects.

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

CI-988 hemihydrate Chemical Structure

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Other Forms of CI-988 hemihydrate:

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

CI-988 inhibits specific ¹²⁵I-BH-CCK-8 binding to NCI-H727 cells with high affinity (K_i 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].

MedChemExpress (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].

MedChemExpress (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

623.74

Formula

C₃₅H₄₂N₄O₆.1/2H₂O

Appearance

Solid

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.[1/2].O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 62.374 mg/mL (100.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6032 mL	8.0162 mL	16.0323 mL
5 mM	0.3206 mL	1.6032 mL	3.2065 mL
10 mM	0.1603 mL	0.8016 mL	1.6032 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6032 mL	8.0162 mL	16.0323 mL	40.0808 mL
	5 mM	0.3206 mL	1.6032 mL	3.2065 mL	8.0162 mL
	10 mM	0.1603 mL	0.8016 mL	1.6032 mL	4.0081 mL
	15 mM	0.1069 mL	0.5344 mL	1.0688 mL	2.6721 mL
	20 mM	0.0802 mL	0.4008 mL	0.8016 mL	2.0040 mL
	25 mM	0.0641 mL	0.3206 mL	0.6413 mL	1.6032 mL
	30 mM	0.0534 mL	0.2672 mL	0.5344 mL	1.3360 mL
	40 mM	0.0401 mL	0.2004 mL	0.4008 mL	1.0020 mL
	50 mM	0.0321 mL	0.1603 mL	0.3206 mL	0.8016 mL
	60 mM	0.0267 mL	0.1336 mL	0.2672 mL	0.6680 mL
	80 mM	0.0200 mL	0.1002 mL	0.2004 mL	0.5010 mL

CI-988 hemihydrate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CI-988 hemihydratePD134308 hemihydrateCholecystokinin ReceptorCCK ReceptorCCK-8CCK2RERKEGFRphosphorylationCa2+anxiolyticanti-tumorInhibitorinhibitorinhibit

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