[CAS NO. 2098546-05-3] EBI-2511
PRODUCTS SPECIFICATIONS [2098546-05-3]
DESCRIPTION [2098546-05-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 576.77 |
| Molecular Formula | C34H48N4O4 |
| SMILES | CCC1=C(C(NCC2=C(C)C=C(C)NC2=O)=O)C(C=C(C3CCN(C(C)C)CC3)O4)=C4C=C1N(C5CCOCC5)CC |
Summary
EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC 50 of 6 nM in Pfeffiera cell lines, respectively.
IC50 & Target
IC50: 6 nM (EZH2) [1] .
In Vitro
EBI-2511 (Compound 34) significantly reduces cellular H3K27me3 levels in a dose-dependent manner with an approximate IC 50 of 8 nM, which is 3-fold more potent than EPZ-6438. In addition to Pfeffier cell line, EBI-2511 was shown active with IC 50 value of 55 nM against WSU-DLCL2 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
EBI-2511 displays a dose-dependent inhibition on the tumor growth, resulting in 28% (10mg/kg), 83% (30mg/kg), and 97% (100mg/kg) reduction in tumor size. At the same dosage level, EBI-2511 shows a superior anti-tumor efficacy to EPZ-6438 (P<0.01). It is noteworthy that no significant changes in body weights of all treatment groups are observed [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 5 mg/mL ( 8.67 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7338 mL | 8.6690 mL | 17.3379 mL |
| 5 mM | 0.3468 mL | 1.7338 mL | 3.4676 mL |
| 10 mM | --- | --- | --- |
