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.

NCT-503 Chemical Structure

NCT-503 Chemical Structure

CAS No. 1916571-90-8

Purity & Quality Control

NCT-503 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-468 Function assay Inhibition of PHGDH in human MDA-MB-468 cells assessed as decrease in serine flux, EC50 = 2.3 μM. 29555419
MDA-MB-468 Cytotoxicity assay Cytotoxicity against human MDA-MB-468 cells, EC50 = 8 μM. 29555419
Click to View More Cell Line Experimental Data

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
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].

In Vivo
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].

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

Chemical Information & Solubility

Molecular Weight 408.48 Formula

C20H23F3N4S

CAS No. 1916571-90-8 SDF Download NCT-503 SDF
Smiles CC1=CC(=NC(=C1)NC(=S)N2CCN(CC2)CC3=CC=C(C=C3)C(F)(F)F)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 81 mg/mL ( (198.29 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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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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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