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NCT-503 

Cat. No.: HY-101966 Purity: 98.40%
Handling Instructions

NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 µM.

For research use only. We do not sell to patients.

NCT-503 Chemical Structure

NCT-503 Chemical Structure

CAS No. : 1916571-90-8

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10 mM * 1 mL in DMSO USD 79 In-stock
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5 mg USD 72 In-stock
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10 mg USD 114 In-stock
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25 mg USD 252 In-stock
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50 mg USD 432 In-stock
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100 mg USD 708 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 µM.

IC50 & Target

IC50: 2.5 µM (PHGDH)[1]

In Vitro

Human phosphoglycerate dehydrogenase (PHGDH) catalyzes the first, rate-limiting step in the canonical glucose-derived serine synthesis pathway. NCT-503, a PHGDH inhibitor, inhibits serine synthesis from 3-phosphoglycerate in cells (IC50=2.5 µM). NCT-503 is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs. Competition studies of NCT-503 against 3-phosphoglycerate (3-PG) and the co-substrate NAD+ reveal a non-competitive mode of inhibition with respect to both 3-PG and NAD+. NCT-503 has EC50s of 8–16 µM for the PHGDH-dependent cell lines, a 6- to 10-fold higher EC50 for MDA-MB-231 cells, and no toxicity towards other PHGDH-independent cell lines[1].

In Vivo

NCT-503 exhibits favorable absorption, distribution, metabolism and excretion (ADME) properties. NCT-503 has good exposure, half-life (2.5 hr) and Cmax (20 µM in plasma) following intraperitoneal administration with significant partitioning into the liver and brain. NCT-503 treatment reduces the growth and weight of PHGDH-dependent MDA-MB-468 xenografts but does not affect the growth or weight of PHGDH-independent MDA-MB-231 xenografts[1].

Molecular Weight

408.48

Formula

C₂₀H₂₃F₃N₄S

CAS No.

1916571-90-8

SMILES

S=C(N1CCN(CC2=CC=C(C(F)(F)F)C=C2)CC1)NC3=NC(C)=CC(C)=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (122.41 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4481 mL 12.2405 mL 24.4810 mL
5 mM 0.4896 mL 2.4481 mL 4.8962 mL
10 mM 0.2448 mL 1.2241 mL 2.4481 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.12 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.12 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Chronic catheters are surgically implanted into the jugular veins of normal or tumor bearing animals 3-4 days prior to infusions. Following administration of either vehicle or NCT-503 at 30 mg/kg, a constant infusion of U-13C-glucose (30 mg/kg/min) is administered for a 3-hour duration. Animals are terminally anesthetized with sodium pentobarbital and all tissues are fully harvested in less than 5 minutes to preserve the metabolic state. Tumors and adjacent lung tissue are carefully dissected and rapidly frozen for analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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NCT-503
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