1844849-10-0
1844849-10-0 structure
- Name: PF-06821497
- Chemical Name: PF-06821497
- CAS Number: 1844849-10-0
- Molecular Formula: C22H24Cl2N2O5
- Molecular Weight: 467.34
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2019-06-02 12:13:56
- Modify Date: 2024-01-03 09:12:40
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PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition[1].
| Name | PF-06821497 |
|---|
| Description | PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition[1]. |
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| Related Catalog | |
| Target |
Ki: <0.1 nM (Y641N EZH2)[1]. |
| In Vivo | PF-06821497 (compound 23a: 100 mg/kg, PO twice daily for 31 days) treatment results in significant inhibition of tumor growth, and the the tumor regressition effect can be sustained for another 40 days after the terminal administration[1]. PF-06821497 with the dose of 300 mg/kg has minimal impact on animal body weights[1]. Animal Model: Mice bearing Karpas-422 DLBCL tumor xenografts (which contain the Y641N EZH2 mutation)[1]. Dosage: 100 mg/kg and 300 mg/kg. Administration: PO twice daily for 31 days. Result: 100 mg/kg dose resulted in significant inhibition of tumor growth and 300 mg/kg dose minimal effected animal body weights. |
| References |
| Molecular Formula | C22H24Cl2N2O5 |
|---|---|
| Molecular Weight | 467.34 |