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NCT-503

CAS No. : 1916571-90-8

MCE 国际站：NCT-503

产品活性：NCT-503磷酸甘油酸脱氢酶 (PHGDH) 抑制剂，IC₅₀ 值为2.5 µM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphoglycerate Dehydrogenase (PHGDH)

In Vitro: NCT-503, a PHGDH inhibitor, inhibits serine synthesis from 3-phosphoglycerate in cells (IC₅₀=2.5 μM). NCT-503 is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs. Competition studies of NCT-503 against 3-phosphoglycerate (3-PG) and the co-substrate NAD⁺ reveal a non-competitive mode of inhibition with respect to both 3-PG and NAD⁺. NCT-503 has EC₅₀s of 8–16 μM for the PHGDH-dependent cell lines, a 6- to 10-fold higher EC₅₀ for MDA-MB-231 cells, and no toxicity towards other PHGDH-independent cell lines.

In Vivo: NCT-503 exhibits favorable absorption, distribution, metabolism and excretion (ADME) properties. NCT-503 has good exposure, half-life (2.5 hr) and C_max (20 μM in plasma) following intraperitoneal administration with significant partitioning into the liver and brain. NCT-503 treatment 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.

相关产品：Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Targeted Diversity Library  |  Heterocyclic Compound Library  |  PHGDH-inactive  |  PKUMDL-WQ-2101  |  NCT-502  |  PHGDH-IN-2  |  BI-4924  |  CBR-5884  |  PHGDH-IN-3  |  PKUMDL-WQ-2201

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