CD 161 ( CD161;CD-161 )

Catalog No. M12418 CAS No. 1627716-22-6

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Product Name

CD 161
Note

Research use only, not for human use.
Brief Description

A potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively.
Description

A potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively; shows high affinity for BRD2, BRD3, BRD4 and BRDT bromodomains, and liitle to no affintiy for other bromodomains (Ki>500 nM); exhibits cytotoxicity against a panel of breast cancer cell lines (MDA-MB-231 IC50=244 nM), demonstrates significant antitumor activity in the MV4;11 leukemia and MDA-MB-231 triple-negative breast cancer xenograft models in mice, has excellent microsomal stability and good oral pharmacokinetics in rats and mice.
Synonyms

CD161;CD-161
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

Cancer
Indication

——

CAS Number

1627716-22-6
Formula Weight

435.49
Molecular Formula

C26H21N5O2
Purity

>98% (HPLC)
Solubility

——
SMILES

CC1=C(C2=CC3=C(C=C2OC)C4=C(C5=CC=NC6=CC=CC=C56)N=C(C)N=C4N3)C(C)=NO1
Chemical Name

4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole

1. Zhao Y, et al. J Med Chem. 2017 May 11;60(9):3887-3901.

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