ButanaMide, N-(3-azidopropyl)-4-[3-[6-(4-Methyl-1-piperazinyl)[2,6'-bi-1H-benziMidazol]-2'-yl]phenoxy]-

Biological Activity

Targapremir-210 (TGP-210) is a potent and selective miR-210 inhibitor. It can inhibits pre-miR-210 processing with high affinity (Kd~200 nM).

in vitro

Targapremir-210 decreases mature miR-210 levels in MDA-MB-231 cells cultured under hypoxic conditions, with an IC ₅₀ of～200 nM.
It (200 nM) induces apoptosis in MDA-MB-231 cells is selective for the hypoxic environment. Targapremir-210 induces apoptosis in cells under hypoxic conditions and does not induce apoptosis in MDA-MB-231 cells cultured in normoxia.

in vivo

Targapremir-210 (100 μL of 200 nM; single ip injection) impedes MDA-MB-231 triple negative breast cancer (TNBC) cells proliferation in vivo. It is able to reach the tumor and sustain for the entire 21-day period, and decreases tumor burden in a TNBC mouse model.

target

storage

Store at -20°C