产品
编 号：F518517
分子式：C22H19N3O4S
分子量：421.47
分子式：C22H19N3O4S
分子量：421.47
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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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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结构图
CAS No: 915412-67-8
产品详情
生物活性：
LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM. LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research.
体内研究：
LP-261 (oral gavage; 4 mg/kg; single dose) displays rapid adsorption by the oral route (Tmax=2.0 h), the terminal half-life of 1.4 h ( 0.2 h indicated a moderate rate of elimination in rat, and the volume of distribution (Vss) is 1.25 L/kg.LP-261 (oral gavage; 15 or 50 mg/kg; twice daily; 28 days) at 50mg/kg results in an approximately tumor volume of 130 mm3 versus 3769 mm3 in the vehicle treated group, this represents a 96% reduction in mean tumor volume. Meanwhile, LP-261 at 15 mg/kg leads to a 41% inhibition after 28 days in this mouse model.Animal Model:Human tumor xenograft model (Injected with NCI-H522 human non-small-cell) in NCr-nu mice
Dosage:15 or 50 mg/kg
Administration:Oral gavage; 15 or 50 mg/kg; twice daily; 28 days
Result:Had potent anti-tumor efficacy at high dosage and exhibited no significant changes in body weights.
体外研究：
LP-261 shows potent G2/M block activity in multiple cell lines and exhibits a range of activity from 0.01μM to 0.38 μM across the tested cell lines, the IC50 values for MCF-7, H522, Jurkat, SW-620, BXPC-3, and PC-3 values are 0.01 μM, 0.01 μM, 0.02 μM, 0.05 μM, 0.05μM and 0.07 μM, respectively.LP-261 exhibits low micromolar potency in the tubulin polymerization assay, the EC50 value of LP-261 is 5.0 μM. LP-261 has the ability to compete with colchicine for binding to tubulin in a[3H]colchicine competition binding assay, the EC50 (3.2 μM) for LP-261 to inhibit the binding with a potency similar to that of colchicine itself, and it exhibits a 79% inhibition at a conctration of 30 μM.
LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM. LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research.
体内研究：
LP-261 (oral gavage; 4 mg/kg; single dose) displays rapid adsorption by the oral route (Tmax=2.0 h), the terminal half-life of 1.4 h ( 0.2 h indicated a moderate rate of elimination in rat, and the volume of distribution (Vss) is 1.25 L/kg.LP-261 (oral gavage; 15 or 50 mg/kg; twice daily; 28 days) at 50mg/kg results in an approximately tumor volume of 130 mm3 versus 3769 mm3 in the vehicle treated group, this represents a 96% reduction in mean tumor volume. Meanwhile, LP-261 at 15 mg/kg leads to a 41% inhibition after 28 days in this mouse model.Animal Model:Human tumor xenograft model (Injected with NCI-H522 human non-small-cell) in NCr-nu mice
Dosage:15 or 50 mg/kg
Administration:Oral gavage; 15 or 50 mg/kg; twice daily; 28 days
Result:Had potent anti-tumor efficacy at high dosage and exhibited no significant changes in body weights.
体外研究：
LP-261 shows potent G2/M block activity in multiple cell lines and exhibits a range of activity from 0.01μM to 0.38 μM across the tested cell lines, the IC50 values for MCF-7, H522, Jurkat, SW-620, BXPC-3, and PC-3 values are 0.01 μM, 0.01 μM, 0.02 μM, 0.05 μM, 0.05μM and 0.07 μM, respectively.LP-261 exhibits low micromolar potency in the tubulin polymerization assay, the EC50 value of LP-261 is 5.0 μM. LP-261 has the ability to compete with colchicine for binding to tubulin in a[3H]colchicine competition binding assay, the EC50 (3.2 μM) for LP-261 to inhibit the binding with a potency similar to that of colchicine itself, and it exhibits a 79% inhibition at a conctration of 30 μM.
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