EZH2-IN-4
EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity.
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- CAS No.: 2088132-99-2
- Formule: C29H41N3O3S
- Masse moléculaire:511.72
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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
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Activité biologique
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WT 5-mer EZH2 0.923 nM (IC50) |
mut 5-mer EZH2 2.65 nM (IC50) |
EZH2-IN-4 (example 38) shows a cell H3K27me3 IC50 of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells[1].
EZH2-IN-4 shows an IC50 of 10.1 nM in Plate Kj«pas-422 cells[1].
EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC50s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC50>20 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2088132-99-2
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Masse moléculaire 511.72
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Formule C29H41N3O3S
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SMILES
CC1=C([C@@H]([C@@]2([H])CC[C@@](N3CC(C3)OC)([H])CC2)C)SC(CCCN4CC5=C(C=C(NC5=O)C)C)=C1C4=O
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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)
EZH2-IN-4 Related Classifications
HY-139150 Related Classifications
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