| Catalog Number： |
E08500 |
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CAS No.: |
1598383-40-4 |
| MDL: |
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Formula: |
C35H51N5O4 ·HCl · H2O |
| F.W.: |
660.3 |
|
Purity: |
99％ |
| Package: |
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Unit: |
mg |
| Appearance: |
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M.P.: |
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| B.P.: |
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Density: |
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| Optical Rotation: |
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Refractive Index: |
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| Solubility: |
Soluble in DMSO |
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Stability: |
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| Storage: |
Store at 0°C (short term), -20°C (long term) |
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Category: |
Reference Standard |
| Reference: |
J. E. Campbell, et al, EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity, ACS Med Chem Lett. 2015 Mar 4;6 (5):491-495 |
| Application: |
EPZ011989 is a cell permeable, metabolically stable and orally available EZH2 inhibitor, a compound with oral exposure and metabolic stability that is able to elicit robust methyl mark inhibition and antitumor activity. It binds potently and selectively to the mutant and wild-type EZH2 with Ki values < 3 nM, and highly selective over closely-related EZH1 (>15-fold selectivity) and 20 other histone methyltransferases (HMTs) (>3000-fold selectivity) tested. Demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. Reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with IC50s below 100 nM. |
| Category: |
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