LP-261 是一种新型的微管蛋白靶向抗癌剂，可与微管蛋白上的秋水仙碱位点结合，诱导 G2/M 期阻滞，其EC50为 3.2 μM。它可抑制人非小细胞肺癌的生长，可用于癌症研究。

LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2/M arrest.

LP-261 was tested as a single agent in colon adenocarcinoma (SW620) and prostate cancer (LNCaP and PC3) xenografts, evaluating several different dosing schedules. LP-261 was also used in combination with bevacizumab in the SW620 xenograft model. LP-261 also exhibited high oral bioavailability and apparent lack of efflux by intestinal transporters such as ABCB1. LP-261 is a very potent inhibitor of angiogenesis, preventing microvessel outgrowth in the rat aortic ring assay and HUVEC cell proliferation at nanomolar concentrations. Complete inhibition of tumor growth was achieved in the PC3 xenograft model and shown to be schedule dependent. Excellent inhibition of tumor growth in the SW620 model was observed, comparable with paclitaxel[1].

LP-261 significantly inhibits growth of a human non-small-cell lung tumor (NCI-H522) in a mouse xenograft model[2].

915412-67-8

C44H36N6O8S2

840.92

DMSO:22 mg/ml (52.20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years