Uses
3-(3-Aminopropoxy)-N-[2-[[3-[[(4-chloro-2-hydroxyphenyl)amino]carbonyl]-2-naphthalenyl]oxy]ethyl]-2-naphthalenecarboxamide Hydrochloride has been identified as an antitumor agent.
Biological Activity
CREB inhibitor (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription with IC50 of 81 nM. It also inhibits the growth of cancer cells without affecting normal cells.
in vitro
666-15 can effectively inhibit the growth of cancer cells. In MDA-MB-231 and MDA-MB-468 cells, the GI50 values of 666-15 were 73 nM and 46 nM, respectively. 666-15 also had strong activity in A549 and MCF-7 cells, with GI50 of 0.47 μM and 0.31 μM, respectively. 666-15 inhibits the transcriptional activity of CREB in live cells that do not depend on direct CREB or CBP binding reactions.
in vivo
In the in vivo MDA-MB-468 xenograft tumor model, 666-15 completely inhibited tumor growth without obvious toxicity. Intraperitoneal injection of 10 mg/kg of 666-15 in mice was well tolerated.
target
| Target | Value |
CREB
() | 81 nM |
