CI-988 hemihydrate
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.
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- Formel: C35H42N4O6.1/2H2O
- Molecular Weight:623.74
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice injected with LoVo cells[3]
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Dosage:10 mg/kg
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Administration:p.o.; daily; for 20 days
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Result:Inhibited the growth of xenografts by 53%.
Chemical Information
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Appearance Solid
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Molecular Weight 623.74
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Formel C35H42N4O6.1/2H2O
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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
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Synonyms
PD134308 hemihydrate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
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.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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
HY-105226B Related Classifications
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