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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] |
Dose | Mice: 40 mg/kg[2] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 1916571-90-8 |
分子式 | C20H23F3N4S |
分子量 | 408.484 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
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 |