中文名：NCT-503
英文名：NCT-503
英文别名：1-Piperazinecarbothioamide, N-(4,6-dimethyl-2-pyridinyl)-4-[[4-(trifluoromethyl)phenyl]methyl]-
纯度：10mM in DMSO
货号：N408855
包装：1ml
Cas号：1916571-90-8
存储温度：-80℃储存
产品介绍：
Information
NCT-503 NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with the IC50 value of 2.5 μM. It is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs.
In vitro
NCT-503 has reasonable aqueous solubility, and exhibits favorable absorption, distribution, metabolism and excretion (ADME) properties. NCT-503 selectively blocks glucose-derived serine synthesis but at the same time triggers SHMT1-dependent one-carbon unit wasting to synthesize serine from glycine. This futile cycle depletes the cell of nucleotides and leads to cell cycle arrest.
In vivo
NCT-503 has good exposure (AUClast=14,700 hr*ng/mL), half-life (2.5 hr) and Cmax (~20 µM in plasma) following intraperitoneal administration with significant partitioning into the liver and brain. PHGDH inhibition by NCT-503 selectively increases necrosis in MDA-MB-468 xenografts, but not in MDA-MB-231 xenografts. It also reduces the growth and weight of PHGDH-dependent MDA-MB-468 xenografts but does not affect the growth or weight of PHGDH-independent MDA-MB-231 xenografts.
Cell Data
cell lines：Sal2, BT474, N87, KPL-4, HCC202, HCC1954, HCC1419, AU565, ZR-75-30, MDA-MB-175, GEO, PC9, A2780 and MRC5
Concentrations：
Incubation Time：
Powder Purity:≥99%
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关键字： 1-?Piperazinecarbothioa?mide, N-?(4,?6-?dimethyl-?2-?pyridinyl)?-?4-?[[4-?(trifluoromethyl)?phenyl]?methyl]?-
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