1049722-30-6
中文名稱
TARGAPREMIR-210
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
化合物 T16991 英文別名
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
物理化學(xué)性質(zhì)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 250 mg/mL (421.81 mM)
形態(tài)Solid
顏色Light yellow to yellow
常見問題列表
生物活性
Targapremir-210 (TGP-210) 是一種有效的、選擇性的 miR-210 抑制劑。 Targapremir-210 以高親和力抑制 pre-miR-210 的加工 (Kd~200 nM)。靶點(diǎn)
IC50: 200 nM (miR-210, in MDA-MB-231 cells).
體外研究
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.
體內(nèi)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. |