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Triapine

CAS No. : 143621-35-6

MCE 站：Triapine

产品活性：Triapine (3-AP; PAN-811) 是一种核糖核苷酸还原酶 (ribonucleotide reductase，RR) 的 M2 亚基抑制剂，是有效的放射致敏剂。

研究领域：Cell Cycle/DNA Damage

作用靶点：DNA/RNA Synthesis

In Vitro: Triapine (3-AP; PAN-811) is a potent derivative of α-heterocyclic carboxaldehyde thiosemicarbazone (HCT) that inhibits hRRM2 ａnd p53R2 isoforms of the M2 subunit. Triapine (3-AP; PAN-811) is thought to inhibit ribonucleotide reductase through its preformed iron chelate, rather than directly by removing iron from the active site. In cells containing less topoisomerase IIα fewer DNA strand breaks will be produced, ａnd thus topoisomerase II poisons will be less inhibitory in the K/VP.5 cell line. The IC₅₀s for Dp44mT growth inhibition are 48±9 nM ａnd 60±12 nM, for K562 ａnd K/VP.5 cells, respectively. The IC₅₀s for Triapine growth inhibition are 476±39 nM ａnd 661±69 nM for K562 ａnd K/VP.5 cells, respectively. PKIH ａnd DpT Fe chelators show high antiproliferative activity against a range of tumor cell lines. Dp44mT shows the greatest antitumor efficacy with an IC₅₀ that ranged from 0.005 to 0.4 μM. The average IC₅₀ of Dp44mT over 28 cell types is 0.03±0.01 μM, which is significantly lower than that of Triapine (3-AP; PAN-811; average IC₅₀: 1.41±0.37 μM).

In Vivo: Triapine (3-AP; PAN-811) causes a significant increase (1.7-fold) in splenic weight when expressed as a percentage of total body weight (1.02±0.06%; n=25) compared with control mice (0.6±0.03%; n=27). In the long-term group, a significant increase in heart weight is observed after Dp44mT (0.4 mg/kg per day) (0.8±0.06%; n=4) compared with control mice (0.5±0.01%; n=6). A significant decrease in the expression of Ndrg1, TfR1, ａnd VEGF1 in the liver is noted for Dp44mT- ａnd Triapine (12 mg/kg per day)-treated animals. The decreased expression could be related to the increased liver Fe in both Dp44mT- ａnd Triapine-treated mice.

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