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LP-261

CAS No. : 915412-67-8

MCE 站：LP-261

产品活性：LP-261 是一种有效的具有口服活性的抗有丝分裂剂 (antimitotic agent)，对体外微管蛋白聚合有抑制作用，其 EC₅₀ 为 3.2 μM。LP-261 在体内可抑制人非小细胞肺癌 (NCI-H522) 的生长，可用于癌症研究。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton

作用靶点：Microtubule/Tubulin

In Vitro: 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.

In Vivo: LP-261 (oral gavage; 4 mg/kg; single dose) displays rapid adsorption by the oral route (T_max=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 (V_ss) 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.

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