Cas No.: | 1627716-22-6 |
Chemical Name: | 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole |
Synonyms: | CD161;CD-161 |
Formula: | C26H21N5O2 |
M.Wt: | 435.487 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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. |