aladdin 阿拉丁 N408855 NCT-503 1916571-90-8 10mM in DMSO

中文名：NCT-503

英文名：NCT-503

英文别名：1-​Piperazinecarbothioa​mide, 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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