EBI-2511
Names
[ CAS No. ]:
2098546-05-3
[ Name ]:
EBI-2511
Biological Activity
[Description]:
EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
[Related Catalog]:
[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 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].
[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].
[References]
[Related Small Molecules]
(+)-JQ1
|
GSK126
|
Tazemetostat (EPZ-6438)
|
Birabresib (OTX015)
|
A 485
|
Curcumin
|
ARV-771
|
ARV-825
|
I-BET762
|
BI 2536
|
GSK343
|
C646
|
3-Deazaneplanocin A (hydrochloride)
|
I-BET151
|
666-15
Chemical & Physical Properties
[ Molecular Formula ]:
C34H48N4O4
[ Molecular Weight ]:
576.77
[ Storage condition ]:
2-8℃