2426665-56-5
2426665-56-5 structure
- Name: Tubulin polymerization-IN-13
- Chemical Name: Tubulin polymerization-IN-13
- CAS Number: 2426665-56-5
- Molecular Formula: C20H21NO6
- Molecular Weight: 371.38
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2022-10-11 18:19:49
- Modify Date: 2024-01-02 06:11:43
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Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity[1].
| Name | Tubulin polymerization-IN-13 |
|---|
| Description | Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity[1]. |
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| Related Catalog | |
| Target |
IC50: 0.37 μM (tubulin polymerization)[1] |
| 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 GI50 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. |
| 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. |
| References |
| Molecular Formula | C20H21NO6 |
|---|---|
| Molecular Weight | 371.38 |