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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $35 | In Stock | |
5 mg | $57 | In Stock | |
10 mg | $92 | In Stock | |
25 mg | $197 | In Stock | |
50 mg | $357 | In Stock | |
100 mg | $556 | In Stock | |
200 mg | $772 | In Stock | |
1 mL x 10 mM (in DMSO) | $63 | In Stock |
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) |
Alias | NCT 503 |
Molecular Weight | 408.48 |
Formula | C20H23F3N4S |
Cas No. | 1916571-90-8 |
Smiles | Cc1cc(C)nc(NC(=S)N2CCN(Cc3ccc(cc3)C(F)(F)F)CC2)c1 |
Relative Density. | 1.306 g/cm3 (Predicted) |
Storage | Powder: -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 (183.61 mM), Sonication is recommended. DMSO: 18.33 mg/mL (44.87 mM), Sonication is recommended. ![]() | ||||||||||||||||||||||||||||||||||||||||
In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1.83 mg/mL (4.48 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.![]() | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Ethanol
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