[(3-氨基吡啶-2-基)亚甲基氨基]硫脲
中文名称 | [(3-氨基吡啶-2-基)亚甲基氨基]硫脲 |
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中文同义词 | 3-氨基吡啶-2-甲醛氨基硫脲腙;2-[(3-氨基吡啶-2-基)亚甲基]氨基硫脲;PAN-811)是核糖核苷酸还原酶抑制剂,已进入各种临床实验。;M2亚基抑制剂(TRIAPINE) |
英文名称 | 3-AP |
英文同义词 | 3-Apct;C078157;Pan 811;Pan811;Pan-811;Triapine;2-((3-AMinopyridin-2-yl)Methylene)hydrazinecarbothioaMide;NSC 663249 |
CAS号 | 143621-35-6 |
分子式 | C7H9N5S |
分子量 | 195.24 |
EINECS号 | |
相关类别 | 小分子抑制剂;小分子抑制剂,天然产物;细胞生物学试剂;标准品;Inhibitors;API |
Mol文件 | 143621-35-6.mol |
结构式 |
[(3-氨基吡啶-2-基)亚甲基氨基]硫脲 性质
熔点 | 234 °C |
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沸点 | 436.0±55.0 °C(Predicted) |
密度 | 1.46±0.1 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | DMSO:可溶10Meq/mL,澄清 |
酸度系数(pKa) | 10.93±0.70(Predicted) |
形态 | 粉末 |
颜色 | 白色至浅棕色 |
CAS 数据库 | 143621-35-6 |
Ribonucleotide reductase (RR)
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).
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.
安全信息
危险品标志 | Xn |
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危险类别码 | 22-36/37/38 |
安全说明 | 26 |
危险品运输编号 | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
海关编码 | 2933.39.6190 |
毒性 | LDLo ivn-rat: 20 mg/kg IJTOFN 19,85,2000 |
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-10082 | [(3-氨基吡啶-2-基)亚甲基氨基]硫脲 3-AP | 143621-35-6 | 5 mg | 520元 |
2024/08/19 | HY-10082 | [(3-氨基吡啶-2-基)亚甲基氨基]硫脲 3-AP | 143621-35-6 | 10 mM * 1 mLin DMSO | 572元 |