(R)-GNE-140

(R)-GNE-140 是一种有效的乳酸脱氢酶 A (LDHA) 抑制剂，对 LDHA 和 LDHB 的 IC50 分别为 3 nM 和 5 nM； (R)-GNE-140 的效力是 S 对映体的 18 倍。

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库存: 现货

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5mg

￥1687.00

1350.00

- +
10mg

￥2850.00

2280.00

- +
50mg

￥8350.00

6680.00

- +
100mg

￥11750.00

9400.00

- +

已选 0 种 0 瓶

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货号: ajci22266
CAS: 2003234-63-5
别名: (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
分子式: C25H23ClN2O3S2
分子量: 499.04
纯度: >98%
溶解度: DMSO : ≥ 14.43 mg/mL (28.92 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.

(R)-GNE-140 inhibits proliferation in 37 of 347 cancer cell lines tested at a potency cut off of 5 uM. (R)-GNE-140 shows inhibitory effect on two chondrosarcoma (bone) cancer cell lines that harbor IDH1 mutations, with IC50 of 0.8 uM[1].

(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.

参考文献:
[1]. Purkey HE, et al. Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. ACS Med Chem Lett. 2016 Aug 26;7(10):896-901.