NCT-503

Catalog No.S8619

For research use only.

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.

NCT-503 Chemical Structure

CAS No. 1916571-90-8

Selleck's NCT-503 has been cited by 4 Publications

Purity & Quality Control

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Biological Activity

Description 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.
Targets
PHGDH [1]
(Cell-free)
2.5 μM
In vitro

NCT-503 has reasonable aqueous solubility, and exhibits favorable absorption, distribution, metabolism and excretion (ADME) properties[1]. 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[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-468 MVLGeY5kfGmxbjDhd5NigQ>? M{L3W2lvcGmkaYTpc44hd2ZiUFjHSGghcW5iaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDz[ZJqdmViZnz1fEwhTUN3MDC9JFIvOyEQvF2u NWnReVRUOjl3NUW0NVk>
MDA-MB-468 NWnGbJdLS3m2b4TvfIlkcXS7IHHzd4F6 M3OwS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20Olgh[2WubIOsJGVEPTBiPTC4JO69VS5? M2PuR|I6PTV3NEG5
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[1].

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: NOD.SCID mice bearing MDA-MB-231 and MDA-MB-468 orthotropic xenografts
  • Dosages: 40 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 408.48
Formula

C20H23F3N4S

CAS No. 1916571-90-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=NC(=C1)NC(=S)N2CCN(CC2)CC3=CC=C(C=C3)C(F)(F)F)C

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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