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NCT-502 Sale

目录号 : GC16860

A PHGDH inhibitor

NCT-502 Chemical Structure

Cas No.:1542213-00-2

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1mg
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5mg
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10mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

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产品描述

IC50: 3.7 μM

NCT-502 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH).

Serine, a proteinogenic amino acid, is the source of one-carbon units essential for de novo purine and deoxythymidine synthesis. Homo sapiens phosphoglycerate dehydrogenase (PHGDH) catalyzes the first, rate-limiting step in the canonical pathway of glucose-derived serine synthesis.

In vitro: NCT-502 was identified as an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells. NCT-502 was inactive against a panel of other dehydrogenases and showed minimal cross-reactivity in a panel of 168 G-protein-coupled receptors. Moreover, In MDA-MB-231-PHGDH cells, NCT-502 treatment could decrease the intracellular serine and glycine concentrations and did not change the concentration of any other amino acid except for aspartate. In addition, NCT-502-mediated inhibition of serine synthesis was found to be reversible in cells [1].

In vivo: To evaluate the in-vivo activity NCT-503, a structurally close analog of NCT-502, 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 reduced the growth and weight of PHGDH-dependent MDA-MB-468 xenografts but did not affect those of PHGDH-independent MDA-MB-231 xenografts. PHGDH inhibition caused by NCT-503 also selectively increased necrosis in MDA-MB-468 but not MDA-MB-231 xenografts. Importantly, mice treated with NCT-503 did not lose weight during the 24-d treatment [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).

Chemical Properties

Cas No. 1542213-00-2 SDF
化学名 N-(4,6-dimethyl-2-pyridinyl)-4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinecarbothioamide
Canonical SMILES S=C(N1CCN(C2=NC=C(C(F)(F)F)C=C2)CC1)NC3=NC(C)=CC(C)=C3
分子式 C18H20F3N5S 分子量 395.4
溶解度 ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide 储存条件 Store at -20°C
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1 mM 2.5291 mL 12.6454 mL 25.2908 mL
5 mM 0.5058 mL 2.5291 mL 5.0582 mL
10 mM 0.2529 mL 1.2645 mL 2.5291 mL
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