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CAS No.: 1916571-90-8

NCT-503 Catalog No. CSN22318

Synonyms: NCT-503

NCT-503 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells with an IC50 value of 2.5 µM.1 It has been shown to reduce the production of glucose-derived serine in cells and to suppress the growth of PHGDH-dependent MDA-MB-468 cancer cells both in vitro and in mice bearing orthotopic xenograft tumors

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述NCT-503 is a PHGDH inhibitor with IC50 value of 2.5μM, and exhibits less potency on PHGDH C234S. It reduced the production of glucose-derived serine in cells. Inhibition of PHGDH reduced the incorporation into nucleotides of one-carbon units from glucose-derived and exogenous serine. NCT-503 showed selective and dose-dependent anti-proliferation on cells expressing PHGDH on high level, including HT1080, HCC70, BT-20, MDA-MB-468 and MT-3, at concentration ranging in 1-30μM. Consistent with this, administration of NCT-503 at dose of 40 mg/kg, i.p., daily reduced tumor growth of MDA-MB-468 orthotopic xenografts in vivo, accompanied with decreased production of glucose-derived serine but no changes in intratumoral serine concentrations.
作用机制NCT-503 can bind to the PHGDH active site at cysteine 234.^[1]
动物研究
剂量
Mice: 40 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 40 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Pacold ME, Brimacombe KR, et al. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol. 2016 Jun;12(6):452-8.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4481 mL
- 12.2404 mL
- 24.4808 mL
- 5 mM
- 0.4896 mL
- 2.4481 mL
- 4.8962 mL
- 10 mM
- 0.2448 mL
- 1.2240 mL
- 2.4481 mL

技术信息

CAS号

1916571-90-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H23F3N4S

运输

蓝冰

分子量

408.48

别名

NCT-503

溶解度

DMSO	220.0 mg/mL (538.6 mM)
Water	insoluble

动物实验配方

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