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Tubulin inhibitor 1

Catalog No.GC33291

Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.

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Tubulin inhibitor 1 Chemical Structure

Cas No.: 2237054-53-2

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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 2237054-53-2 SDF
Canonical SMILES CCOC1=CC=C(C2=CN(C)N=C2C3=CC(OC)=C(OC)C(OC)=C3)C=C1
Formula C21H24N2O4 M.Wt 368.43
Solubility DMSO : ≥ 125 mg/mL (339.28 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.7142 mL 13.5711 mL 27.1422 mL
5 mM 0.5428 mL 2.7142 mL 5.4284 mL
10 mM 0.2714 mL 1.3571 mL 2.7142 mL
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