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Tubulin polymerization-IN-13

Tubulin polymerization-IN-13

产品编号 T61482   CAS 2426665-56-5

Tubulin polymerization-IN-13 (Compound 4f) is a potent inhibitor of tubulin polymerization, with an IC50 value of 0.37 μM. It displays significant anti-proliferative effects against cancer cells, inducing apoptosis and exhibiting potential antivascular activity [1].

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Tubulin polymerization-IN-13 Chemical Structure
Tubulin polymerization-IN-13, CAS 2426665-56-5
规格 价格/CNY 货期 数量
25 mg ¥ 10,600 6-8周
50 mg ¥ 13,800 6-8周
100 mg ¥ 17,500 6-8周
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: Tubulin polymerization-IN-13 (T61482)
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产品描述 Tubulin polymerization-IN-13 (Compound 4f) is a potent inhibitor of tubulin polymerization, with an IC50 value of 0.37 μM. It displays significant anti-proliferative effects against cancer cells, inducing apoptosis and exhibiting potential antivascular activity [1].
体外活性 Tubulin polymerization-IN-13 (0.005-2.8 nM) treatment inhibits tumor cell proliferation [1]. Tubulin polymerization-IN-13 (8.7-10 μM) is non-toxic in non-tumor cells [1]. Tubulin polymerization-IN-13 (1-50 nM; 24 h) treatment induces cell cycle arrest in G2/M [1]. Tubulin polymerization-IN-13 (10 nM; 24 and 48 h) treatment induces cell apoptosis [1]. Tubulin polymerization-IN-13 (10-100 nM; 24 h) treatment induces alteration of the microtubule network [1]. Cell Proliferation Assay [1] Cell Line: HeLa, HT-29, Daoy, HL-60, SEM, and Jurkat cells Concentration: 0.005-2.8 nM Incubation Time: Result: Showed IC 50 s of 2.8 nM, 2.1 nM, 0.005 nM, 2.7 nM, 0.31 nM, and 0.28 nM for HeLa, HT-29, Daoy, HL-60, SEM, and Jurkat cells, respectively. Cell Cytotoxicity Assay [1] Cell Line: Peripheral blood lymphocytes (PBL) Concentration: 8.7-10 μM Incubation Time: Result: Showed a GI 50 of 8.7 μM in quiescent lymphocytes. Cell Cycle Analysis [1] Cell Line: HeLa cells Concentration: 1, 5, 10, and 50 nM Incubation Time: 24 hours Result: Induced a G2/M arrest at 10 nM, increased G2/M cells accompanied by a strong reduction of cells in the G1 phase. Apoptosis Analysis [1] Cell Line: HeLa cells Concentration: 10 nM Incubation Time: 24 and 48 hours Result: Induced caspase-9 activation, PARP cleavage, Bcl-2 phosphorylation and Mcl-1 downregulation. Immunofluorescence [1] Cell Line: HeLa cells Concentration: 10, 50, and 100 nM Incubation Time: 24 hours Result: Showed the disorganization of microtubules at 10 nM, and much more evident at 50 and 100 nM.
体内活性 Tubulin polymerization-IN-13 (intraperitoneal injection; 15 or 5 mg/kg; once every other day; 4 times) reduces tumor growth in a dose-dependent manner in an orthotopic murine tumor model [1]. Animal Model: Seven-week-old C57BL/6 female mice orthotopically injected into the mammary fat pad with E0771 mammary carcinoma cells [1] Dosage: 15 or 5 mg/kg Administration: Intraperitoneal injection; 15 or 5 mg/kg; once every other day; 4 times Result: Reduced tumor mass by 45.7% and 16.9% at 15 and 5 mg/kg, respectively. Showed no sign of toxicity and no decreasement in animal body weight.
分子量 371.38
分子式 C20H21NO6
CAS No. 2426665-56-5

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

Tubulin polymerization-IN-13 2426665-56-5 Inhibitor inhibitor inhibit

 

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