| Name | NCT-503 |
| 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. |
| 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) |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.83 mg/mL (4.48 mM), Solution.
Ethanol : 75 mg/mL (183.61 mM), Sonication is recommended.
DMSO : 127 mg/mL (310.91 mM), Sonication is recommended.
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| Keywords | TAMReceptor | TAM Receptor | PHGDH(Cell-free) | NCT-503 | NCT503 | Inhibitor | inhibit | FLT3 | AXL |
| Inhibitors Related | Mycophenolate Mofetil | Rotenone | Ribavirin | 18β-Glycyrrhetinic acid | Benzyl alcohol | Sorafenib | 2-Methylaminoethanol | Methotrexate disodium | Dimethyl malonate | Isomalt | D-Mannitol | Ethyl potassium malonate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Hematonosis Compound Library | Angiogenesis related Compound Library | Inhibitor Library | NO PAINS Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Fluorochemical Library |
United States
