中文名：NCT-503
英文名：NCT-503
英文別名：1-?Piperazinecarbothioa?mide, N-?(4,?6-?dimethyl-?2-?pyridinyl)?-?4-?[[4-?(trifluoromethyl)?phenyl]?methyl]?-
純度：10mM in DMSO
貨號(hào)：N408855
包裝：1ml
Cas號(hào)：1916571-90-8
存儲(chǔ)溫度：-80℃儲(chǔ)存
產(chǎn)品介紹：
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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關(guān)鍵字： 1-?Piperazinecarbothioa?mide, N-?(4,?6-?dimethyl-?2-?pyridinyl)?-?4-?[[4-?(trifluoromethyl)?phenyl]?methyl]?-
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