1049722-30-6
中文名称
TARGAPREMIR-210
英文名称
ButanaMide, N-(3-azidopropyl)-4-[3-[6-(4-Methyl-1-piperazinyl)[2,6'-bi-1H-benziMidazol]-2'-yl]phenoxy]-
CAS
1049722-30-6
分子式
C32H36N10O2
分子量
592.694
MOL 文件
1049722-30-6.mol
1049722-30-6 结构式
基本信息
中文别名
化合物 T16991 英文别名
Targapremir-210ButanaMide, N-(3-azidopropyl)-4-[3-[6-(4-Methyl-1-piperazinyl)[2,6'-bi-1H-benziMidazol]-2'-yl]phenoxy]-
N-(3-azidopropyl)-4-(4-(6-(4-methylpiperazin-1-yl)-1H,3'H-[2,5'-bibenzo[d]imidazol]-2'-yl)phenoxy)butanamide
N-(3-azidopropyl)-4-[3-[6-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-benzimidazol-2-yl]phenoxy]butanamide
常见问题列表
生物活性
Targapremir-210 (TGP-210) 是一种有效的、选择性的 miR-210 抑制剂。 Targapremir-210 以高亲和力抑制 pre-miR-210 的加工 (Kd~200 nM)。靶点
IC50: 200 nM (miR-210, in MDA-MB-231 cells).
体外研究
Targapremir-210 decreases mature miR-210 levels in MDA-MB-231 cells cultured under hypoxic conditions, with an IC
50
of ∼200 nM.
Targapremir-210 (200 nM) induces MDA-MB-231 cells apoptosis is selective for the hypoxic environment. Targapremir-210 induces cells apoptosis under hypoxic conditions and does not induce apoptosis in MDA-MB-231 cells cultured in normoxia.
体内研究
Targapremir-210 (100 μL of 200 nM; single i.p. injection) impedes MDA-MB-231 triple negative breast cancer (TNBC) cells proliferation in vivo. Targapremir-210 is able to reach the tumor and sustain for the entire 21-day period, and decreases tumor burden in a TNBC mouse model.
| Animal Model: | NOD/SCID mice were subcutaneously transplanted cell suspension into breast fat pads. |
| Dosage: | 100 μL of 200 nM |
| Administration: | Single i.p. injection 24 h post-transplantation |
| Result: | Decreased tumor growth as assessed by luciferase signal intensity and mass of the resected tumor. |