产品说明书

NCT-503

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Chemical Structure| 1916571-90-8 同义名 : -
CAS号 : 1916571-90-8
货号 : A380274
分子式 : C20H23F3N4S
纯度 : 99%+
分子量 : 408.484
MDL号 : MFCD30343875
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(122.4 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 12.5 mg/mL(30.6 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
靶点

  • Dehydrogenase

    PHGDH, IC50:2.5 μM
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.24mL

12.24mL

2.45mL

1.22mL

24.48mL

4.90mL

2.45mL
参考文献

[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.