NCT-503

SKU: orb1303056

Description

NCT-503 is a selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=2.5 µM) with demonstrated antitumor activity. It is used in cancer metabolism research to suppress the growth of PHGDH-dependent tumors in both cellular and animal models.

Research Area

Cardiovascular Research, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 1916571-90-8
• MW: 408.48
• Formula: C₂₀H₂₃F₃N₄S
• SMILES: Cc1cc(C)nc(NC(=S)N2CCN(Cc3ccc(cc3)C(F)(F)F)CC2)c1
• Target: FLT|||Dehydrogenase|||TAM Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1.83 mg/mL (4.48 mM);Ethanol:75 mg/mL (183.61 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:127 mg/mL (310.91 mM)

Bioactivity

• Target IC50:
  PHGDH:2.5 μM
• 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.
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• 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. 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PHGDH(Cell-free), TAMReceptor, TAM Receptor, Inhibitor, FLT3, NCT 503, NCT503, NCT-503, inhibit, AXL

Compound Identifiers

PubChem CID

118796328