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(R)-GNE-140
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
(R)-GNE-140图片
CAS NO:2003234-63-5
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
(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。
Cas No.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
化学名(13E,14E,22R,6R)-35-fluoro-6-methyl-7-aza-1(5,3)-pyrazolo[1,5-a]pyrimidina-3(3,2)-pyridina-2(1,2)-pyrrolidinacyclooctaphan-8-one
Canonical SMILESO=C1N[C@@](C2=CSC=C2)(C3=CC=C(N4CCOCC4)C=C3)CC(O)=C1SC5=CC=CC=C5Cl
分子式C25H23ClN2O3S2
分子量499.04
溶解度DMSO : ≥ 14.43 mg/mL (28.92 mM);Water :< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

(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.

References:
[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.