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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
EI1 (KB-145943; EI-1) is a potent and selective inhibitor of EZH2 (Enhancer of zeste homolog 2) with potential antitumor activity. It inhibits EZH2 (WT) and EZH2 (Y641F) with an IC50 of 15 nM and 13 nM, respectively.
ln Vitro |
EI1 (KB-145943) is known to suppress cellular H3K27 methylation and promote the expression of the Ezh2 target gene p16 in DLBCL cells. Moreover, EI1 (KB-145943) suppresses H3K27me3 and cell division in mouse embryonic fibroblasts. Furthermore, EI1 (KB-145943) induces cell cycle arrest and apoptosis in DLBCL cells that possess the Ezh2 mutation, while also specifically inhibiting their growth[1].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Qi W, et al. Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21360-5
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Molecular Formula |
C23H26N4O2
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Molecular Weight |
390.48
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CAS # |
1418308-27-6
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Related CAS # |
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SMILES |
O=C(C1C([H])=C(C#N)C([H])=C2C=1C([H])=C([H])N2C([H])(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])N([H])C([H])([H])C1C(N([H])C(C([H])([H])[H])=C([H])C=1C([H])([H])[H])=O
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5610 mL | 12.8048 mL | 25.6095 mL | |
5 mM | 0.5122 mL | 2.5610 mL | 5.1219 mL | |
10 mM | 0.2561 mL | 1.2805 mL | 2.5610 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.