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详细内容
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Tubulin inhibitor 1 is a tubulin inhibitor, occupying the colchicine binding site, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis[1].
Tubulin inhibitor 1 (Compound 7a3) is a tubulin inhibitor, occupying the colchicine binding site, inhibits tubulin polymerization[1].Tubulin inhibitor 1 has potent anti-proliferative activity against SK-OV-3, MDA-MB-231, HeLa, A549, CT26 and MCF-7 cells, with IC50s of 16.7 ± 3.0, 31.4 ± 0.7, 32.8 ± 2.9, 67.0 ± 0.8, 58.0 ± 2.4 and 35.4 ± 5.6 nM, respectively[1].Tubulin inhibitor 1 (40, 80, and 160 nM, 48 hours) markedly causes cellular mitotic arrest in the G2/M phase, induces apoptosis in SK-OV-3 cells[1].|| Apoptosis Analysis[1]||Cell Line:|SK-OV-3 cells|Concentration:|40, 80, and 160 nM|Incubation Time:|48 h|Result:|Induced apoptosis in SK-OV-3 cells after treatment for 48 h.
Tubulin inhibitor 1 (50 mg/kg, i.p., every two days three times for 20-25 days) is well tolerated, significantly reduces tumour growth in Balb/c nude mice bearing SK-OV-3 cells[1].|| Animal Model:|Six-week-old Balb/c nude mice (18-20 g) beraring SK-OV-3 cells[1]|Dosage:|50 mg/kg|Administration:|I.P., every two days three times for 20-25 days|Result:|Significantly reduced tumour growth in Balb/c nude mice bearing SK-OV-3 cells, without obvious body weight loss.
[1]. Lai Q, et al. Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site. Eur J Med Chem. 2018 Aug 5;156:162-179.
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