NCT-503

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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。

CAS NO:

1916571-90-8

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议

产品介绍

化学性质

Storage	Store at -20°C
M.Wt	408.5
Cas No.	1916571-90-8
Formula	C₂₀H₂₃F₃N₄S
Solubility	≥40.9 mg/mL in DMSO; insoluble in H2O; ≥20.33 mg/mL in EtOH
Chemical Name	N-(4,6-dimethyl-2-pyridinyl)-4-[[4-(trifluoromethyl)phenyl]methyl]-1-piperazinecarbothioamide
Canonical SMILES	S=C(N1CCN(CC2=CC=C(C(F)(F)F)C=C2)CC1)NC3=NC(C)=CC(C)=C3
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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).