PF-06726304 acetate
Based on 1 publication(s) in Google Scholar
PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity.
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- CAS. Nr.: 2080306-28-9
- Formel: C24H25Cl2N3O5
- Molecular Weight:506.38
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) PF-06726304 acetate
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
EZH2 WT 0.7 nM (Ki) |
EZH2 Y641N 3.0 nM (Ki) |
In Vitro
PF-06726304 (Compound 31) inhibits H3K27me3 in Karpas-422 with an IC50 of 15 nM[1].
PF-06726304 inhibits the proliferation of Karpas-422 cells that harbor wild-type EZH2 with an IC50 of 25 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Scid beige mice (6-8 weeks old) with Karpas-422 xenograft model[1]
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Dosage:200 and 300 mg/kg
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Administration:Given BID for 20 days
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Result:Inhibited tumor growth and induced robust modulation of downstream biomarkers in a subcutaneous Karpas-422 xenograft model.
Chemical Information
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CAS. Nr. 2080306-28-9
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Molecular Weight 506.38
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Formel C24H25Cl2N3O5
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SMILES
O=C1N(CC2=C(C)C=C(C)NC2=O)CCC3=C1C(Cl)=C(C4=C(C)ON=C4C)C=C3Cl.CC(O)=O
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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.
Publications (1)
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Journal Impact Factor
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Most Recent
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Front Cell Dev Biol
EZH2/EHMT2 Histone Methyltransferases Inhibit the Transcription of DLX5 and Promote the Transformation of Myelodysplastic Syndrome to Acute Myeloid Leukemia. [Abstract]2021 Aug 2:9:619795. PMID: 34409024
Reinheit & Dokumentation
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Calculators
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