BETd-246

Research use only, not for human use.

A potent, second-generation BET protein degrader that exhibits superior selectivity, potency and antitumor activity.

A potent, second-generation BET protein degrader that exhibits superior selectivity, potency and antitumor activity; completely and selectively depletes BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation; displays strong growth inhibition and apoptosis induction activity in TNBC cell lines with IC50 <1 uM, induces a rapid and time-dependent downregulation of MCL1 protein; decreases BET proteins in xenograft breast tumors and suppress tumor growth in vivo without causing weight loss.

BETd 246;BETd246

PROTACs

PROTAC

PROTAC

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2140289-17-2

946.04

C48H55N11O10

>98% (HPLC)

DMSO : 200 mg/mL 211.41 mM

CCN1C(=CC(=N1)C2CC2)NC3=NC(=NC4=C3C5=CC(=C(C=C5N4)C6=C(ON=C6C)C)OC)C(=O)NCCCOCCOCCOCCCNC7=CC=CC8=C7C(=O)N(C8=O)C9CCC(=O)NC9=O

4-((3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino)-7-(3,5-dimethylisoxazol-4-yl)-N-(3-(2-(2-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)propoxy)ethoxy)ethoxy)propyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years