Tubulin-inhibitor-1 - Tubulin 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETubulin inhibitor 1Cat. No.: HY-112607CAS No.: 2237054-53-2分式: CHNO分量: 368.43作靶点: Microtubule/Tubulin; Apoptosis作通路: Cell Cycle/DNA Damage; Cytoskeleton; Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1

2、month溶解性数据体外实验 DMSO : 125 mg/mL (339.28 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7142 mL 13.5711 mL 27.1422 mL5 mM 0.5428 mL 2.7142 mL 5.4284 mL10 mM 0.2714 mL 1.3571 mL 2.7142 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的

3、溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.65 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.65 mM); Clear solu

4、tion3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (5.65 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Tubulin inhibitor 1tubulin 抑制剂，靶作于秋仙素结合位点，抑制微管蛋聚集。Tubulin inhibitor 1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 1。IC50 & Target Tubulin 1体外研究 Tubulin

5、 inhibitor 1 (Compound 7a3) is a tubulin inhibitor, occupying the colchicine binding site, inhibits tubulinpolymerization 1.Tubulin inhibitor 1 has potent anti-proliferative activity against SK-OV-3, MDA-MB-231, HeLa, A549, CT26and MCF-7 cells, with IC50s of 16.7 3.0, 31.4 0.7, 32.8 2.9, 67.0 0.8, 5

6、8.0 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 1Cell Line: SK-OV-3 cellsConcentration: 40, 80, and 160 nMIncubation Time: 48 hResult: Induced a

7、poptosis in SK-OV-3 cells after treatment for 48 h.体内研究 Tubulin inhibitor 1 (50 mg/kg, i.p., every two days three times for 20-25 days) is well tolerated, significantlyreduces 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-

8、OV-3 cells 1Dosage: 50 mg/kgAdministration: I.P., every two days three times for 20-25 daysResult: Significantly reduced tumour growth in Balb/c nude mice bearing SK-OV-3 cells, withoutobvious body weight loss.REFERENCES1. Lai Q, et al. Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site. Eur J MedChem. 2018 Aug 5;156:162-179.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has not been fully validated for medical appli