产品
编 号：F756360
分子式：C26H34N2O
分子量：390.56
分子式：C26H34N2O
分子量：390.56
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CAS No: 2851480-01-6
产品详情
生物活性：
Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 μM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity.
体内研究：
Keap1-Nrf2-IN-4 (50, 100 mg/kg; i.g.; per day for 21 days) exhibits antitumor activity on xenograft model without obvious side effect.Animal Model:5-6 weeks, 18-20 g, NOD SCID mice (xenograft tumor model)
Dosage:50, 100 mg/kg
Administration:i.g.; per day, 21 days
Result:Exihibited good antitumor activity on xenograft model without obvious side effect.
体外研究：
Keap1-Nrf2-IN-4 (compound 4g) (72 h) shows anti-proliferation activity (IC50 s of 2.55, 3.88, 3.74, 2.89 μM in MGC-803, MCF-7, A549, HepG-2 cells, respectively).Keap1-Nrf2-IN-4 inhibits neddylation of cullin1, cullin3, cullin5.Keap1-Nrf2-IN-4 blocks the migration ability of MGC-803 without cell cycle arrest.Keap1-Nrf2-IN-4 (24, 48 h) induces apoptosis of MGC-803 and HGC-27 cells in concentration- and time-dependent manners.
Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 μM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity.
体内研究：
Keap1-Nrf2-IN-4 (50, 100 mg/kg; i.g.; per day for 21 days) exhibits antitumor activity on xenograft model without obvious side effect.Animal Model:5-6 weeks, 18-20 g, NOD SCID mice (xenograft tumor model)
Dosage:50, 100 mg/kg
Administration:i.g.; per day, 21 days
Result:Exihibited good antitumor activity on xenograft model without obvious side effect.
体外研究：
Keap1-Nrf2-IN-4 (compound 4g) (72 h) shows anti-proliferation activity (IC50 s of 2.55, 3.88, 3.74, 2.89 μM in MGC-803, MCF-7, A549, HepG-2 cells, respectively).Keap1-Nrf2-IN-4 inhibits neddylation of cullin1, cullin3, cullin5.Keap1-Nrf2-IN-4 blocks the migration ability of MGC-803 without cell cycle arrest.Keap1-Nrf2-IN-4 (24, 48 h) induces apoptosis of MGC-803 and HGC-27 cells in concentration- and time-dependent manners.
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