BET inhibitor CF53 ( —— )

Catalog No. M12767 CAS No. 1808160-52-2

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Product Name

BET inhibitor CF53
Note

Research use only, not for human use.
Brief Description

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

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.
Synonyms

——
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

——
Indication

——

CAS Number

1808160-52-2
Formula Weight

443.51
Molecular Formula

C24H25N7O2
Purity

>98% (HPLC)
Solubility

DMSO : 110 mg/mL 248.03 mM
SMILES

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

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

1. Zhao Y, et al. J Med Chem. 2018 Jul 17. doi: 10.1021/acs.jmedchem.8b00483.

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