EHT-6706 free base
EHT-6706 free base is a tubulin inhibitor with an IC50 value of 1 μM against porcine tubulin. EHT-6706 free base binds to the colchicine-binding site on tubulin to inhibit tubulin polymerization and disrupt the cellular microtubule network. EHT-6706 free base acts as an antiproliferative, vascular-disrupting, permeability-modulating, migration-inhibiting and antiangiogenic agent. EHT-6706 free base exhibits inhibitory activity against human tumor cells. EHT-6706 free base can be used in cancer and angiogenesis research.
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- CAS. Nr.: 1351592-10-3
- Formel: C21H24N2O4
- Molecular Weight:368.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
EHT-6706 (4 h) free base binds to the Colchicine (HY-16569)-binding site on porcine tubulin with an IC50 of 0.17 μM[1].
EHT-6706 (10 nM-50 nM; 24 h) free base disrupts the intracellular microtubule network of HCT116 cells in a concentration-dependent manner[1].
EHT-6706 (0.0003 μM-10 μM; 72 h) free base potently inhibits the proliferation of 60 human tumor cell lines (e.g., T47D, HT-29, A498, A549), with an IC50 range of 0.3 nM to 11.6 nM after 72 hours of treatment[1].
EHT-6706 (10 nM-100 nM; 18 h) free base inhibits capillary lumen formation by HUVEC on Matrigel, with an IC50 of 22 nM calculated by total lumen length and an IC50 of 15 nM calculated by the number of branching points[1].
EHT-6706 (1 nM-100 nM; overnight) free base disrupts the pre-established capillary tube structures formed by HUVEC on Matrigel[1].
EHT-6706 (10 nM-100 nM; 15 min) free base increases the permeability of confluent HUVEC monolayers in a dose-dependent manner[1].
EHT-6706 (10 nM-1 μM; 1 h) free base alters the morphology of HUVEC and disrupts the stability of the F-actin cytoskeleton, with prominent vesicular protrusions observable[1].
EHT-6706 (10 nM-100 nM; 22 h) free base inhibits FGF-2- and VEGF-induced HUVEC migration in a concentration-dependent manner, with the maximum inhibitory effect achieved after treatment with 100 nM for 22 hours[1].
EHT-6706 (40 nM; 18 h) free base causes abnormal regulation of expression levels in 3364 genes by ≥2-fold, most of which are upregulated anti-angiogenic genes, with a subset being downregulated pro-angiogenic genes, while also increasing the level of TLL-1 protein in cell supernatants[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:10, 25, 50 nM
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Incubation Time:24 h
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Result:Caused only slight microtubule and nuclear alterations at 10 nM.
Induced condensed chromatin, decreased tubulin immunoreactivity, and disordered microtubule distribution at 25 nM.
Triggered major morphological changes including loss of adhesion, cell rounding, and very weak microtubular immunoreactivity at 50 nM.
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Cell Line:HUVEC
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Concentration:10 nM, 100 nM, 1 μM
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Incubation Time:1 h
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Result:Induced cell blebbing with actin accumulation around membrane micelle-like protrusions at 100 nM.
Caused further morphological disruption at 1 μM.
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Cell Line:HUVEC
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Concentration:10, 50, 100 nM
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Incubation Time:22 h
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Result:Caused concentration-dependent inhibition of HUVEC migration toward both FGF-2 and VEGF.
Achieved near-complete inhibition at 100 nM.
Chemical Information
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CAS. Nr. 1351592-10-3
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Molecular Weight 368.43
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Formel C21H24N2O4
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SMILES
NC1=C(OCC)C=CC2=C1C=NC=C2CC3=CC(OC)=C(OC)C(OC)=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)