产品
编 号：F113268
分子式：C35H42N4O6
分子量：614.73
分子式：C35H42N4O6
分子量：614.73
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CAS No: 130332-27-3
产品详情
生物活性：
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.
体内研究：
CI-988 (10 mg/kg; p.o.; daily; for 20 days) inhibits the growth of colorectal cancer in xenografts model mice.Animal Model:Nude mice injected with LoVo cells
Dosage:10 mg/kg
Administration:p.o.; daily; for 20 days
Result:Inhibited the growth of xenografts by 53%.
体外研究：
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+. 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.
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.
体内研究：
CI-988 (10 mg/kg; p.o.; daily; for 20 days) inhibits the growth of colorectal cancer in xenografts model mice.Animal Model:Nude mice injected with LoVo cells
Dosage:10 mg/kg
Administration:p.o.; daily; for 20 days
Result:Inhibited the growth of xenografts by 53%.
体外研究：
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+. 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.
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