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Cat. No. M8604
NCT-503 Structure


Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 70  USD70 In stock
10mg USD 100  USD100 In stock
25mg USD 190  USD190 In stock
100mg USD 475  USD475 In stock
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Quality Control & Documentation
Biological Activity

NCT-503 is an inhibitor of phosphoglycerate dehydrogenase (PHGDH), which catalyzes the first, rate-limiting step of glucose-derived serine synthesis. NCT-503 reduced glucose-derived serine production and suppressed the growth of both PHGDH-dependent cancer cells in culture and in xenograft tumors, and caused G1/S cell cycle arrest in MDA-MB-468 cells. NCT-503 reduced the incorporation of one-carbon units from glucose-derived and exogenous serine into nucleotides, which may contribute to its anticancer activity. NCT-503 had an IC50 value of 2.5 μM for PHGDH and was inactive against a panel of other dehydrogenases and minimal cross-reactivity in a panel of 168 G-protein-coupled receptors (GPCRs). NCT-503 was found to be noncompetitive with respect to both 3-PG and NAD+, and exhibit good stability (>98% after 48 hrs in assay buffer) and aqueous solubility.

Protocol (for reference only)
Cell Experiment
Cell lines MDA-MB-468, BT-20, MT-3 cells
Preparation method MDA-MB-468, BT-20, MT-3 cells are seeded in white 96-well plates allowed to attach for 24 hours. Cells are treated with NCT-503 for four days. Cell viability is assessed with Cell Titer-Glo and luminescence measured with a plate reader.
Incubation time 4 days
Animal Experiment
Animal models Female NOD.CB17-Prkdcscid/J mice
Formulation 5% ethanol, 35% PEG 300, and 60% of an aqueous 30% hydroxypropyl-β-cyclodextrin solution
Administration injected intraperitoneally once daily
Chemical Information
Molecular Weight 408.48
Formula C20H23F3N4S
CAS Number 1916571-90-8
Solubility (25°C) DMSO 45 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Pacold ME, et al. Nat Chem Biol. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate.

Related PHGDH Products

PKUMDL-WQ-2101 is a non-NAD+-competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 34.8 μM. PKUMDL-WQ-2101 exhibits antitumor activity.


PHGDH-inactive has no activity against PHGDH and serves as a negative control of NCT-502 and NCT-503.


NCT-502 is a human phosphoglycerate dehydrogenase (PHGDH) inhibitor, cytotoxic to PHGDH-dependent cancer cells, and reduces glucose-derived serine production, with an IC50 of 3.7 μM against PHGDH.


BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability.


BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD+-competitive PHGDH inhibitor.

Abmole Inhibitor Catalog

Keywords: NCT-503, NCT503 supplier, PHGDH, inhibitors, activators

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