Tubulin polymerization-IN-13 (Compound 4f) 是一种微管蛋白聚集抑制剂 (IC50=0.37 μM) 。Tubulin polymerization-IN-13 表现出对癌细胞的抗增殖活性，可诱导细胞凋亡，具有潜在的抗血管活性。
| 生物活性 | Tubulin polymerization-IN-13 (Compound 4f) is atubulin polymerizationinhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity againstcancercells, inducesapoptosisand potential antivascular activity[1]. |
| IC50& Target | IC50: 0.37 μM (tubulin polymerization)[1] |
体外研究
(In Vitro) | 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 IC50s 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 GI50of 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. |
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体内研究
(In Vivo) | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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