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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
规格:98%
分子量:499.04
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
A TRK kinase (TKI) inhibitor
CAS:2003234-63-5
分子式:C25H23ClN2O3S2
分子量:499.04
纯度:98%
存储:Store at -20°C

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.