Tubulininhibitor1是tubulin抑制剂，靶作用于秋水仙素结合位点，抑制微管蛋白聚集。Tubulininhibitor1具有抗肿瘤活性，能够导致细胞G2/M期有丝分裂停滞，诱导细胞凋亡。
货号:ajcx12972
CAS:2237054-53-2
分子式:C21H24N2O4
分子量：368.43
溶解度:DMSO : ≥ 125 mg/mL (339.28 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.