产品
编 号：F752234
分子式：C42H43N5O8
分子量：745.82
分子式：C42H43N5O8
分子量：745.82
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CAS No: 2411548-90-6
产品详情
生物活性：
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer.
体内研究：
HI5 (15 and 30 mg/kg; IV; daily, for 21 days) significantly inhibits tumor growth at a dose-dependent manner.Animal Model:BALB/c nude mice (18-22 g, 5 week-old, injected with HeLa cells)
Dosage:15 and 30 mg/kg
Administration:IV; daily, for 21 days
Result:Significantly inhibited tumor growth at a dose-dependent manner with inhibitory rates of 50.73% and 65.76% at doses of 15 and 30 mg/kg, respectively.
体外研究：
HI5 (0-10 μM; 72 hours) exhibits potent antiproliferative activity in HeLa, PC-3, A549 and HUVEC.HI5 (0.1 and 0.5 μM; 24 hours) exhibits markedly disruption of microtubule organization in a concentration-dependent manner.HI5 (0.5 μM; 24 hours) significantly up-regulates the expression level of Bax protein, while down-regulates the protein of Bcl-2, furthermore, markedly up-regulates the protein expressions of caspase-3 and PARP.
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer.
体内研究：
HI5 (15 and 30 mg/kg; IV; daily, for 21 days) significantly inhibits tumor growth at a dose-dependent manner.Animal Model:BALB/c nude mice (18-22 g, 5 week-old, injected with HeLa cells)
Dosage:15 and 30 mg/kg
Administration:IV; daily, for 21 days
Result:Significantly inhibited tumor growth at a dose-dependent manner with inhibitory rates of 50.73% and 65.76% at doses of 15 and 30 mg/kg, respectively.
体外研究：
HI5 (0-10 μM; 72 hours) exhibits potent antiproliferative activity in HeLa, PC-3, A549 and HUVEC.HI5 (0.1 and 0.5 μM; 24 hours) exhibits markedly disruption of microtubule organization in a concentration-dependent manner.HI5 (0.5 μM; 24 hours) significantly up-regulates the expression level of Bax protein, while down-regulates the protein of Bcl-2, furthermore, markedly up-regulates the protein expressions of caspase-3 and PARP.
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