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NCT-503

NCT-503
NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=2.5 µM) with no activity against other dehydrogenases. NCT-503 has antitumor activity and inhibits the growth of PHGDH-dependent tumors.
Catalog No. T4213Cas No. 1916571-90-8
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Purity:99.56%
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NCT-503

Purity: 99.56%
Catalog No. T4213Alias NCT 503Cas No. 1916571-90-8

NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=2.5 µM) with no activity against other dehydrogenases. NCT-503 has antitumor activity and inhibits the growth of PHGDH-dependent tumors.
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Pack SizePriceAvailabilityQuantity
2 mg$35In Stock
5 mg$57In Stock
10 mg$92In Stock
25 mg$197In Stock
50 mg$357In Stock
100 mg$587In Stock
200 mg$772In Stock
500 mg$1,190In Stock
1 mL x 10 mM (in DMSO)$63In Stock
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Product Introduction

Bioactivity
Description
NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=2.5 µM) with no activity against other dehydrogenases. NCT-503 has antitumor activity and inhibits the growth of PHGDH-dependent tumors.
Targets&IC50
PHGDH:2.5 μM
In vitro
METHODS: Mouse bone marrow cells (BMC) transformed with MLL-AF9 and Hoxa9/Meis1 (HM-2) were treated with MI-503 (0-5 µM) for 7 days, and viability was measured by MTT assay.
RESULTS: Treatment of MLL-AF9 oncogene-transformed BMC with MI-503 resulted in significant growth inhibition, with a GI50 value of 0.22 µM measured after 7 days of treatment.[1]
METHODS: AGS cells overexpressing wild-type menin and three mutant proteins were treated with MI-503 (1 µmol/L) for 48 h. The expression levels of target proteins were detected by Western Blot.
RESULTS: MI-503 increased the expression of nuclear proteins, with the greatest effect observed in R516fs and E235K mutants. [2]
In vivo
METHODS: To test the in vivo antitumor activity, MI-503 (60 mg/kg, 25% DMSO+25% PEG400+50% PBS) was administered intraperitoneally to BALB/c nude mice bearing MV4;11 xenografts once a day for 20 days.
RESULTS: MI-503 strongly inhibited tumor growth, and treatment with MI-503 resulted in more than 80% reduction of MV4;11, and complete regression of tumor volume and tumor in two mice. [1]
Animal Research
Animal Models: NOD.SCID mice bearing MDA-MB-231 and MDA-MB-468 orthotropic xenograftsFormulation: 5% ethanol, 35% PEG 300, and 60% of an aqueous 30% hydroxypropyl-β-cyclodextrin solutionDosages: 40 mg/kgAdministration: i.p.(Only for Reference)
AliasNCT 503
Chemical Properties
Molecular Weight408.48
FormulaC20H23F3N4S
Cas No.1916571-90-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 75 mg/mL (183.6 mM)
DMSO: 18.33 mg/mL (44.88 mM)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM2.4481 mL12.2405 mL24.4810 mL122.4050 mL
5 mM0.4896 mL2.4481 mL4.8962 mL24.4810 mL
10 mM0.2448 mL1.2241 mL2.4481 mL12.2405 mL
20 mM0.1224 mL0.6120 mL1.2241 mL6.1203 mL
Ethanol
1mg5mg10mg50mg
50 mM0.0490 mL0.2448 mL0.4896 mL2.4481 mL
100 mM0.0245 mL0.1224 mL0.2448 mL1.2241 mL

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