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编 号:F021101
分子式:C32H36N10O2
分子量:592.69
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM). Targapremir-210 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

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.

体外研究:
Targapremir-210 decreases mature miR-210 levels in MDA-MB-231 cells cultured under hypoxic conditions, with an IC50 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.
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