| Size | Price | Stock | Qty |
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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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Purity: ≥98%
EBI-2511 is a novel and orally available benzofuran derived EZH2 inhibitors that was discovered through a scaffold hopping approach based on the clinical compound of EPZ-6438. It has the potential for treatment of Non-Hodgkin’s Lymphoma. Further rational structure-activity relationship exploration and optimization led to the discovery of more potent EZH2 inhibitors with oral bioavailability in mice and rats. EBI-2511 demonstrated excellent in vivo efficacy in Pfeiffer tumor Xenograft models in mouse and is under preclinical development for the treatment of cancers associated with EZH2 mutations.
| ln Vitro |
EBI-2511 (Compound 34) dramatically decreases cellular H3K27me3 levels in a dose-dependent manner with an approximate IC50 of 8 nM, which is 3-fold more effective than EPZ-6438. In addition to Pfeffier cell line, EBI-2511 was found active with IC50 value of 55 nM against WSU-DLCL2[1].
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| ln Vivo |
EBI-2511 has a dose-dependent suppression of tumor growth, leading to a reduction in tumor size of 28% (10 mg/kg), 83% (30 mg/kg), and 97% (100 mg/kg). EBI-2511 outperforms EPZ-6438 in terms of anti-tumor activity at the same dosage level (P<0.01). Notably, there are no appreciable variations in the body weights of any treatment groups[1].
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| Animal Protocol |
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| References |
[1]. Lu B, et al. Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma. ACS Med Chem Lett. 2018 Jan 29;9(2):98-102.
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| Molecular Formula |
C34H48N4O4
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| Molecular Weight |
576.78
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| CAS # |
2098546-05-3
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| Related CAS # |
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| SMILES |
O1C2=CC(N(CC)C3CCOCC3)=C(CC)C(C(NCC3=C(C)C=C(C)NC3=O)=O)=C2C=C1C1CCN(C(C)C)CC1
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| Chemical Name |
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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) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (0.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (0.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (0.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7338 mL | 8.6688 mL | 17.3376 mL | |
| 5 mM | 0.3468 mL | 1.7338 mL | 3.4675 mL | |
| 10 mM | 0.1734 mL | 0.8669 mL | 1.7338 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.
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