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CAS No. : 2760612-63-1
MCE 国际站:Skp2 inhibitor 1
产品活性:Skp2 inhibitor 1(compound 14i) 是一种 Skp2 抑制剂,干扰 Skp2-Cks1 相互作用,IC50为 2.8 μM。Skp2 inhibitor 1 也具有抗癌活性。
研究领域:Metabolic Enzyme/Protease
作用靶点:E1/E2/E3 Enzyme
In Vitro: Skp2 inhibitor 1 (2.8 μM,72 h) interferes the Skp2−Cks1 interaction, against PC-3 and MGC-803 cells with IC50 values of 4.8 and 7.0 μM, respectively.
Skp2 inhibitor 1 (10 μM, 48h) inhibits the proliferation and migration of PC-3 and MGC-803 cell, causing them to block in the S phase and promote cell apoptosis .
In Vivo: Skp2 inhibitor 1 (50 mg/kg, intraperitoneal injection/2 day, 21 days) inhibits tumor growth significantly in NOD-SCID xenograft models without obvious toxicity. In addition, the tumor treated with Skp2 inhibitor 1 (50 mg/Kg/2 day) was completely suppressed in vivo.
Skp2 inhibitor 1 decreases tumor malignancy via suppressing the Skp2 signal pathway and increase the proportion of apoptosis in the tumor tissue.
Pharmacokinetic Parameters of Compound 14i in the Plasma and Tumor Tissue
药代动力学分析
PK parameters | plasma | tumor tissue |
t1/2 | 14.1±1.5(h) | 12.6±7.8(h) |
Cmax | 176.1±30.3(ng/mL) | 182.0±80.9(ng/g) |
AUClast | 3231.5±407.2(h.ng/mL) | 2443.9±474.9(h.ng/g) |
AUCINF | 3551.5±465.3(h.ng/mL) | 2636.0±619.7(h.ng/g) |
VZ | 143.3±9.2(L/kg) | 170.8±80.1(mg/kg) |
CL | 7.1±0.8(L/h/kg) | 15.7±4.2(mg/h/kg) |
MRTlast | 13.4±0.64(h) | 9.9±2.5(h) |
t1/2 of 14i in the Liver Microsomes and Liver S9 ofDifferent Species体外代谢分析
| species | human | rat | mouse |
t1/2 | liver microsomes | 66.0 | 16.3 | 15.3 |
t1/2 | liver S9 | 64.8 | 15.4 | 16.5 |
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