中文名 | CS-2624 |
英文名 | (R)-GNE-140 ;GNE140 |
别名 | 化合物(R)-GNE-140 LDHA抑制剂((R)-GNE-140) (R)-3-((2-氯苯基)硫基)-4-羟基-6-(4-吗啉苯基)-6-(噻吩-3-基)-5,6-二氢吡啶-2(1H)-酮 (6R)-3-[(2-氯苯基)硫代]-5,6-二氢-4-羟基-6-[4-(4-吗啉基)苯基]-6-(3-噻吩基)-2(1H)-吡啶酮 |
英文别名 | GNE140 GNE-140 CS-2624 GNE 140 (R)-GNE-140 (R)-GNE-140 ;GNE140 (R)-GNE-140 (GNE-140 (R)-3-((2-chlorophenyl)thio)-4-hydroxy-6-(4-morpholinophenyl)-6-(thiophen-3-yl)-5,6-dihydropyridin-2(1H)-one 2(1H)-Pyridinone, 3-[(2-chlorophenyl)thio]-5,6-dihydro-4-hydroxy-6-[4-(4-morpholinyl)phenyl]-6-(3-thienyl)-, (6R)- |
CAS | 2003234-63-5 |
化学式 | C25H23ClN2O3S2 |
分子量 | 499.04 |
密度 | 1.46±0.1 g/cm3(Predicted) |
沸点 | 695.4±55.0 °C(Predicted) |
溶解度 | DMSO : 14.43 mg/mL (28.92 mM);H2O : < 0.1 mg/mL (不溶) |
酸度系数 | 4.50±1.00(Predicted) |
存储条件 | 2-8°C(protect from light) |
体外研究 | (R)-GNE-140 inhibits proliferation in 37 of 347 cancer cell lines tested at a potency cut off of 5 μM. (R)-GNE-140 shows inhibitory effect on two chondrosarcoma (bone) cancer cell lines that harbor IDH1 mutations, with IC 50 of 0.8 μM. |
体内研究 | (R)-GNE-140 (5 mg/kg) has high bioavailability in mice. At higher oral doses, ranging from 50 to 200 mg/kg, (R)-GNE-140 displays greater exposure. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.004 ml | 10.019 ml | 20.038 ml |
5 mM | 0.401 ml | 2.004 ml | 4.008 ml |
10 mM | 0.2 ml | 1.002 ml | 2.004 ml |
5 mM | 0.04 ml | 0.2 ml | 0.401 ml |
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