BET inhibitor CF53

Research use only, not for human use.

BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1).

BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1); potently inhibits different BET proteins with Kd values of 0.5-2.2 nM, weakly inhibits CREBBP (Ki=47 nM) and shows excellent selectivity over other bromodomain containing proteins; inhibits cell growth in MOLM-13 and MDA-MB-231 cell lines with IC50 of 7 and 85 nM, respectively; CF53 demonstrates significant antitumor activity in both triple-negative breast cancer and acute leukemia xenograft models in mice.

——

Chromatin/Epigenetic

Bromodomain

Bromodomain

——

——

1808160-52-2

443.51

C24H25N7O2

>98% (HPLC)

DMSO : 110 mg/mL 248.03 mM

CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)NC4=C3C(=NC(=N4)C)NC5=CC(=NN5C)C6CC6)OC

N-(3-Cyclopropyl-1-methyl-1H-pyrazol-5-yl)-7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-2-methyl-9H-pyrimido[4,5-b]indol-4-amine

(-20℃)

With Ice Pack

≥ 2 years