E7974
E7974 is a selective inhibitor of α-tubulin (α-tubulin) with an IC50 of 3.9 μM. E7974 disrupts mitotic spindle formation, induces G2-M phase cell cycle arrest, initiates apoptosis, activates caspase-3, and induces poly (ADP-ribose) polymerase cleavage. E7974 reduces the area of choroidal neovascularization in mouse models, and exerts anti-angiogenic effects when loaded in modified micelles. E7974 can be used in research related to cancer and choroidal neovascularization.
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- CAS No.: 610787-07-0
- Formule: C24H43N3O4
- Masse moléculaire:437.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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α-Tubulin 3.9 μM (IC50) |
E7974 (300 nM; 0-24 h) induces sustained G2-M phase mitotic arrest in human histiocytic lymphoma U-937 cells, thereby triggering apoptosis characterized by the formation of subdiploid cells starting at 8 h post-treatment[1].
E7974 (300 nM; 1-13 h) induces maximal mitotic arrest in human histiocytic lymphoma U-937 cells[1].
E7974 (300 nM; 0-24 h) induces apoptosis in human histiocytic lymphoma U-937 cells, which is confirmed by the cleavage of procaspase-3 and PARP starting at 6 h post-treatment[1].
E7974 (19.5-65 nM; 18 h) disrupts mitotic spindle formation and induces mitotic arrest in DU 145 human prostate cancer cells, and also reduces microtubule density in non-dividing cells at higher concentrations[1].
E7974 (300 nM) induces G2-M phase mitotic arrest and subsequent apoptosis in human prostate cancer cell line DU 145[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U-937 human histiocytic lymphoma cells
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Concentration:300 nM
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Incubation Time:0-24 h
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Result:Induced a G2-M block beginning as early as 4 h of treatment, with the G1 phase completely depleted by 10 h.
Showed an increasing hypodiploid cell population, indicative of apoptosis, evident at 8 h, and nearly all cells were hypodiploid after 24 h.
Demonstrated approximately 80% of U-937 cells in the G2-M peak after 14 h of treatment were positive for phospho-histone H3, confirming mitotic arrest, and close to half of hypodiploid cells were also phospho-histone H3 positive.
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Cell Line:U-937 human histiocytic lymphoma cells
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Concentration:300 nM
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Incubation Time:0, 10, 30, 45, 60 min, followed by 12 h incubation in drug-free medium
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Result:Showed percentages of cells in G2-M after 12 h in drug-free medium were 15% (0 min exposure), 35% (10 min), 47% (30 min), 62% (45 min), and 71% (60 min).
Demonstrated a 60-minute exposure to E7974 was sufficient to induce near-complete mitotic arrest 12 h later.
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Cell Line:U-937 human histiocytic lymphoma cells
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Concentration:300 nM
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Incubation Time:0-24 h
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Result:Induced proteolytic cleavage of procaspase-3 (generating active caspase-3) and PARP (generating an 84 kDa cleaved fragment) after 6 h of exposure, correlating with the appearance of hypodiploid cells detected by flow cytometry.
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Cell Line:DU 145 human prostate cancer cells
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Concentration:19.5 nM, 65 nM
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Incubation Time:18 h
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Result:Induced marked increases in numbers of mitotic cells (positive for phospho-histone H3), with disorganized, tangled arrays of short microtubule fragments forming abnormal mitotic spindles; chromosomes failed to align at the cell center, indicating arrest in late prophase or prometaphase.
Showed at the higher concentration (65 nmol/L), nonmitotic cells had marked decreases in microtubule density.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male, adult, laser-induced choroidal neovascularization)[2]
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Dosage:0.2 µM; 2 µM; 20 µM
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Administration:intravitreal; single dose immediately after laser coagulation
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Result:Did not significantly reduce CNV area compared to vehicle-treated eyes (0.2 µM standalone).
Did not significantly reduce CNV area compared to vehicle-treated eyes (2 µM standalone).
Caused a significant reduction in CNV area compared to vehicle-treated eyes (20 µM standalone).
Chemical Information
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CAS No. 610787-07-0
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Masse moléculaire 437.63
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Formule C24H43N3O4
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SMILES
C(N[C@H](C(N([C@H](/C=C(/C(O)=O)\C)[C@@H](C)C)C)=O)C(C)(C)C)(=O)[C@@H]1N(C(C)C)CCCC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Kuznetsov G, et al. Tubulin-based antimitotic mechanism of E7974, a novel analogue of the marine sponge natural product hemiasterlin. Mol Cancer Ther. 2009;8(10):2852-2860. [Content Brief]
[2]. Takahashi K, et al. Anti-VEGFR2 Antibody-modified Micelle for Triggered Drug Delivery and Effective Therapy of Choroidal Neovascularization. Curr Neurovasc Res. 2019;16(3):258-265. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
E7974 Related Classifications
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