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NCT-503
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。
NCT-503图片
CAS NO:1916571-90-8
规格:98%
分子量:408.5
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
3-phosphoglycerate dehydrogenase (PHGDH) inhibitor
CAS:1916571-90-8
分子式:C20H23F3N4S
分子量:408.5
纯度:98%
存储:Store at -20°C

Background:

IC50: 2.5 μM for inhibiting serine synthesis from 3-phosphoglycerate in cells


NCT-503 is a 3-phosphoglycerate dehydrogenase (PHGDH) inhibitor.


In the canonical pathway of glucose-derived serine synthesis, Homo sapiens phosphoglycerate dehydrogenase (PHGDH) has been reported to catalyze the first, rate-limiting step.


In vitro: NCT-503 was identified as an inhibitor of PHGDH and was found to be inactive against a panel of other dehydrogenases and showed minimal cross-reactivity in a panel of G-protein-coupled receptors. In addition, treatment of three PHGDH-independent cell lines and five PHGDHdependent cell lines with NCT-503 demonstrated that NCT-503 had EC50 values of 8–16 μM for the PHGDH-dependent cell lines, and no toxicity toward other PHGDH-independent cell lines [1].


In vivo: To evaluate NCT-503 in-vivo activity, NOD.SCID mice bearing MDA-MB-231 and MDA-MB-468 orthotopic xenografts were treated with vehicle or NCT-503. Results showed that NCT-503 treatment reduced the growth and weight of PHGDH-dependent xenografts but did not affect those of PHGDH-independent xenografts. Importantly, mice treated with NCT-503 did not lose weight during the 24-d treatment in spite of the potential systemic toxicities of inhibiting serine biosynthesis [1].


Clinical trial: So far, no clinical study has been conducted.


Reference:
[1] Pacold, M. E.,Brimacombe, K.R.,Chan, S.H., et al. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nature Chemical Biology 12(6), 452-458 (2016).