DW532
DW532 is a dual inhibitor of tubulin and tyrosine kinase, with IC50 values of 4.9 μM and 5.5 μM against EGFR and VEGFR2, respectively, and a KD of 3.6 μM for tubulin. DW532 induces cell cycle arrest at the G2/M phase, triggers cell apoptosis via caspase-related pathways, and inhibits angiogenesis. DW532 can be used for research related to cancers (e.g., breast cancer).
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- CAS No.: 1267949-42-7
- Formule: C16H12O6
- Masse moléculaire:300.27
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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
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Activité biologique
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VEGFR2 5.5 μM (IC50) |
EGFR 4.9 μM (IC50) |
C-src 8.6 μM (IC50) |
DW532 (1-10 μM; 2 h) dose-dependently inhibits ligand-induced VEGFR2 activation and its downstream signaling pathways in HUVECs, as well as EGFR activation and its downstream signaling pathways in A431 human epithelial cancer cells[1].
DW532 (10-40 μM; 30 min) is a microtubule destabilizer that inhibits tubulin polymerization in vitro in a dose-dependent manner[1].
DW532 (0.1-10 μM; 12 h) dose-dependently inhibits tubulin polymerization in human breast cancer MDA-MB-468 cells, reduces the level of polymerized tubulin and increases the level of soluble tubulin[1].
DW532 (10 μM; 6 h) disrupts the microtubule network in human lung cancer A549 cells and induces diffuse tubulin staining, which is consistent with the characteristics of microtubule destabilization[1].
DW532 (72 h) potently and non-selectively inhibits the proliferation of a panel of 16 human cancer cell lines, with a mean IC50 of 1.82 μM[1].
DW532 (0.1-10 μM; 6 h) dose-dependently inhibits tube formation in human umbilical vein endothelial cells (HUVECs) in vitro[1].
DW532 (10 μM; 12 h) disrupts mitotic spindle assembly in human lung cancer A549 cells, induces chromosome dispersion and multipolar spindle formation, and rarely causes the appearance of monopolar spindles[1].
DW532 (1-10 μM; 24 h) induces G2/M phase arrest in MDA-MB-468, A549, PC-3, KB, K562 and A431 human cancer cells, accompanied by altered levels of mitosis-related proteins cyclin B1, p-CDK1 and p-H3[1].
DW532 (0.1-20 μM; 48 h) induces dose-dependent apoptosis in KB, MDA-MB-468 and A431 human cancer cells via a caspase-related mechanism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human umbilical vein endothelial cells (HUVECs), A431 human epithelial cancer cells
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Concentration:1, 5 and 10 μM
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Incubation Time:2 h (pre-incubated prior to 15 min ligand stimulation)
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Result:Dose-dependently inhibited VEGF-induced phosphorylation of VEGFR2 and its downstream target Akt in HUVECs.
Similarly inhibited EGF-induced phosphorylation of EGFR and downstream Akt in A431 cells.
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Cell Line:MDA-MB-468 human breast carcinoma cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:12 h
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Result:Dose-dependently decreased polymerized tubulin in pellets and increased soluble tubulin in supernatants, promoting the transition of cellular tubulin from polymerized to free state.
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Cell Line:A549 human lung cancer cells
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Concentration:10 μM
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Incubation Time:6 h
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Result:Disrupted the intact, stretched microtubule network seen in untreated cells, resulting in dispersed tubulin staining similar to that induced by the microtubule destabilizer vincristine (VCR).
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Cell Line:A549 human lung cancer cells
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Concentration:10 μM
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Incubation Time:12 h
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Result:Induced scattered chromosomes in the cytoplasm, formation of multipolar spindles, and a small proportion of monopolar spindles, consistent with traditional microtubule destabilizers.
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Cell Line:KB mouth epidermal carcinoma cells, MDA-MB-468 human breast carcinoma cells, A431 human epithelial carcinoma cells
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Concentration:0.1, 1 and 10 μM (Annexin V/PI); 0.1, 1, 5, 10 and 20 μM (Western Blot)
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Incubation Time:48 h
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Result:Induced dose-dependent apoptosis: ~59.7% of KB cells underwent apoptosis at 1 μM, and ~70% at 10 μM.
Dose-dependently increased cleavage of caspase-3, caspase-9, and PARP, indicating a caspase-related apoptosis mechanism.
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Cell Line:MDA-MB-468, A549, PC-3, KB, K562, and A431 human cancer cells
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Concentration:1 and 10 μM
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Incubation Time:24 h
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Result:Arrested all six tested cell lines at the G2/M phase.
Increased levels of mitotic markers cyclin B1 and p-H3, and decreased levels of phosphorylated (inhibitory) CDK1 (Tyr15).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:fertilized eggs[1]
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Dosage:0.1 nmol per egg; 1 nmol per egg
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Administration:local application
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Result:Significantly inhibited neovascularization at both tested doses compared to untreated controls.
Chemical Information
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CAS No. 1267949-42-7
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Masse moléculaire 300.27
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Formule C16H12O6
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SMILES
O=C1OC=2C(O)=C(O)C=CC2C(=C1)C=3C=CC(OC)=C(O)C3
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DW532 Related Classifications
HY-116068 Related Classifications
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