中文名 | NG 52 |
英文名 | NG 52 |
别名 | 化合物NG-52 CDC28P和PHO85P激酶抑制剂(NG 52) 2-[[6-[(3-氯苯基)氨基]-9-异丙基-9H-嘌呤-2-基]氨基]乙醇 |
英文别名 | NG 52 NG-52 COMPOUND 52 NG 52 (Compound 52 ) 2-(2-HYDROXYETHYLAMINO)-6-(3-CHLORANILINO)-9-ISOPROPYLPURINE 2-(2-HYDROXYETHYLAMINO)-6-(3-CHLOROANILINO)-9-ISOPROPYLPURINE 2-(2-Hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine, NG-52 2-((6-((3-chlorophenyl)aMino)-9-isopropyl-9H-purin-2-yl)aMino)ethanol 2-[[6-[(3-Chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]ethanol |
CAS | 212779-48-1 |
化学式 | C16H19ClN6O |
分子量 | 346.81 |
密度 | 1.42±0.1 g/cm3(Predicted) |
沸点 | 587.7±60.0 °C(Predicted) |
溶解度 | 二氯甲烷: 50毫克/毫升,澄清,无色 |
酸度系数 | 14.54±0.10(Predicted) |
存储条件 | Keep in dark place,Sealed in dry,2-8°C |
外观 | 粉末 |
颜色 | white to off-white |
体外研究 | NG 52 (Compound 52) inhibits growth in a drug-sensitized yeast strain ( S. cerevisiae ) with a GI 50 of 30 μM. NG 52 is active against cdc2-cyclin B with an IC 50 value of 340 nM. NG 52 dose-dependently inhibits the proliferation of glioma U87 and U251 cell lines with GI 50 values of 7.8 μM and 5.2 μM, respectively, meanwhile it potently inhibits the proliferation of primary glioma cells. NG 52 (12.5-50 μM) effectively inhibits the phosphorylation of PDHK1 at Thr338 site and the phosphorylation of PDH at Ser293 site in U87 and U251 cells, resulting in more pyruvic acid entering the Krebs cycle with increased production of ATP and ROS. NG 52 can reverse the Warburg effect by enhancing the activity of pyruvate dehydrogenase (PDH) through inhibiting the activity of PGK1, and switched cellular glucose metabolism from anaerobic mode to aerobic mode. Cell Proliferation Assay Cell Line: Glioma U87 and U251 cells Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM Incubation Time: 6 days Result: Potently inhibited the proliferation of primary glioma cells. Western Blot Analysis Cell Line: Glioma U87 and U251 cells Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM Incubation Time: 12 hours or 24 hours Result: Potently inhibited the proliferation of primary glioma cells. |
体内研究 | NG 52 (50-150 mg/kg; oral administration; daily; for 13 days) treatment dose-dependently suppresses the growth of glioma xenograft. Animal Model: Female nu/nu mice (5-week-old) injected with glioma cells Dosage: 50 mg/kg, 100 mg/kg, 150 mg/kg Administration: Oral administration; daily; for 13 days Result: Dose-dependently suppressed the growth of glioma xenograft. |
危险品标志 | Xn - 有害物品 |
风险术语 | R40 - 少数报道有致癌后果。 R68 - 可能有不可逆后果的危险。 |
安全术语 | 36/37 - 穿戴适当的防护服和手套。 |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.883 ml | 14.417 ml | 28.834 ml |
5 mM | 0.577 ml | 2.883 ml | 5.767 ml |
10 mM | 0.288 ml | 1.442 ml | 2.883 ml |
5 mM | 0.058 ml | 0.288 ml | 0.577 ml |
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