产品
编 号：F315302
分子式：C15H11ClN2OS
分子量：302.78
分子式：C15H11ClN2OS
分子量：302.78
产品类型
规格
价格
是否有货
1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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200mg
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结构图
CAS No: 312636-16-1
产品详情
生物活性：
SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation.
体内研究：
Chronic SKI II (50.0 mg/kg, 3-weekly i.p. for 16 weeks) administration leads to permanent reduction of S1P concentrations in plasma in mice.SKI II (50.0 mg/kg, IP; 100 mg/kg, PO) treatment reduces tumor growth in mice bearing solid tumor model.Animal Model:8 week-old female LDL-R-/- mice.
Dosage:50.0 mg/kg.
Administration:IP injection daily, 3 days a week for 16 weeks.
Result:A single administration of produced a significant reduction of plasma S1P with themaximum (~40%) observed 12 h after injection. At sacrifice (72 h after last injection) S1P levels were 266 ± 18 ng/mL and 328 ± 30 ng/mL in the SKI-II-treated and control groups,respectively.
Animal Model:BALB/c mouse solid tumor model that uses JC mammary adenocarcinoma cells.
Dosage:50.0 mg/kg.
Administration:IP injection daily, 3 days a week for 16 weeks.
Result:Had strong inhibition of tumor growth from the start of treatment of 65%, with no toxicity or weight loss.
Animal Model:BALB/c JC tumor model.
Dosage:100 mg/kg.
Administration:PO every other day.
Result:Caused significant antitumor activity in well-established tumors as early as day 5, with maximal response seen at the end of the study. Showed 79% inhibition of tumor growth from the start of treatment.
体外研究：
SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II promotes the degradation of β-catenin by enhancing Wnt5A.SKI II (1.25 μM, 48 h) in combination with DDP has a clear synergistic effect in human gastric carcinoma SGC7901/DDP cell line.
SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation.
体内研究：
Chronic SKI II (50.0 mg/kg, 3-weekly i.p. for 16 weeks) administration leads to permanent reduction of S1P concentrations in plasma in mice.SKI II (50.0 mg/kg, IP; 100 mg/kg, PO) treatment reduces tumor growth in mice bearing solid tumor model.Animal Model:8 week-old female LDL-R-/- mice.
Dosage:50.0 mg/kg.
Administration:IP injection daily, 3 days a week for 16 weeks.
Result:A single administration of produced a significant reduction of plasma S1P with themaximum (~40%) observed 12 h after injection. At sacrifice (72 h after last injection) S1P levels were 266 ± 18 ng/mL and 328 ± 30 ng/mL in the SKI-II-treated and control groups,respectively.
Animal Model:BALB/c mouse solid tumor model that uses JC mammary adenocarcinoma cells.
Dosage:50.0 mg/kg.
Administration:IP injection daily, 3 days a week for 16 weeks.
Result:Had strong inhibition of tumor growth from the start of treatment of 65%, with no toxicity or weight loss.
Animal Model:BALB/c JC tumor model.
Dosage:100 mg/kg.
Administration:PO every other day.
Result:Caused significant antitumor activity in well-established tumors as early as day 5, with maximal response seen at the end of the study. Showed 79% inhibition of tumor growth from the start of treatment.
体外研究：
SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II promotes the degradation of β-catenin by enhancing Wnt5A.SKI II (1.25 μM, 48 h) in combination with DDP has a clear synergistic effect in human gastric carcinoma SGC7901/DDP cell line.
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