CAS NO: | 2237054-53-2 |
包装 | 价格(元) |
250mg | 电议 |
500mg | 电议 |
Cas No. | 2237054-53-2 |
Canonical SMILES | CCOC1=CC=C(C2=CN(C)N=C2C3=CC(OC)=C(OC)C(OC)=C3)C=C1 |
分子式 | C21H24N2O4 |
分子量 | 368.43 |
溶解度 | DMSO : ≥ 125 mg/mL (339.28 mM) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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. |