中文名 | 3-AP ( PAN-811) |
英文名 | 3-aminopyridine-2-carboxaldehyde thiosemicarbazone |
别名 | 3-氨基吡啶-2-甲醛氨基硫脲腙 M2亚基抑制剂(TRIAPINE) 2-[(3-氨基吡啶-2-基)亚甲基]氨基硫脲 |
英文别名 | 3-Apct Pan811 Pan 811 Pan-811 C078157 Triapine NSC 663249 3-AP ( PAN-811) 3-aminopyridine-2-carboxaldehyde thiosemicarbazone 2-((3-AMinopyridin-2-yl)Methylene)hydrazinecarbothioaMide |
CAS | 143621-35-6 |
化学式 | C7H9N5S |
分子量 | 195.24 |
密度 | 1.46±0.1 g/cm3(Predicted) |
熔点 | 234 °C |
沸点 | 436.0±55.0 °C(Predicted) |
溶解度 | DMSO: soluble10Meq/mL, clear |
酸度系数 | 10.93±0.70(Predicted) |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | white to light brown |
体外研究 | 3-AP (Triapine) is a potent derivative of α-heterocyclic carboxaldehyde thiosemicarbazone (HCT) that inhibits hRRM2 and p53R2 isoforms of the M2 subunit. 3-AP (Triapine) 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 IC 50 s for Dp44mT growth inhibition are 48±9 nM and 60±12 nM, for K562 and K/VP.5 cells, respectively. The IC 50 s for 3-AP 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 IC 50 that ranged from 0.005 to 0.4 μM. The average IC 50 of Dp44mT over 28 cell types is 0.03±0.01 μM, which is significantly lower than that of 3-AP (Triapine; average IC 50 : 1.41±0.37 μM). |
体内研究 | 3-AP (Triapine) 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 3-AP (12 mg/kg per day)-treated animals. The decreased expression could be related to the increased liver Fe in both Dp44mT- and 3-AP-treated mice. |
危险品标志 | Xn - 有害物品 |
风险术语 | R22 - 吞食有害。 R36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | 26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 |
危险品运输编号 | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 5.122 ml | 25.609 ml | 51.218 ml |
5 mM | 1.024 ml | 5.122 ml | 10.244 ml |
10 mM | 0.512 ml | 2.561 ml | 5.122 ml |
5 mM | 0.102 ml | 0.512 ml | 1.024 ml |
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