CAS NO: | 2098546-05-3 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cas No. | 2098546-05-3 |
Canonical 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 |
分子式 | C34H48N4O4 |
分子量 | 576.77 |
溶解度 | DMSO : 5 mg/mL (8.67 mM) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively. EBI-2511 (Compound 34) significantly reduces cellular H3K27me3 levels in a dose-dependent manner with an approximate IC50 of 8 nM, which is 3-fold more potent than EPZ-6438. In addition to Pfeffier cell line, EBI-2511 was shown active with IC50 value of 55 nM against WSU-DLCL2[1]. 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]. [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. |