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Chemical Structure| 1916571-90-8 Chemical Structure| 1916571-90-8

Structure of NCT-503
CAS No.: 1916571-90-8

Chemical Structure| 1916571-90-8

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

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Product Details of NCT-503

CAS No. :1916571-90-8
Formula : C20H23F3N4S
M.W : 408.48
SMILES Code : S=C(N1CCN(CC2=CC=C(C(F)(F)F)C=C2)CC1)NC3=NC(C)=CC(C)=C3
MDL No. :MFCD30343875
InChI Key :PJNSZIQUFLWRLH-UHFFFAOYSA-N
Pubchem ID :118796328

Safety of NCT-503

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315
Precautionary Statements:P264-P280-P302+P352-P332+P313-P362+P364

Isoform Comparison

Biological Activity

Target
  • Dehydrogenase

    PHGDH, IC50:2.5 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
HCC 50 µM 48 h NCT-503 worked synergistically with Sorafenib to induce HCC cell apoptosis. PMC6794322
PC9ER4 cells 25 μM and 50 μM NCT-503 significantly up-regulated the erlotinib sensitivity of PC9ER4 and HCC827ER9 cells. PMC5858502
Huh7 and A52 10, 25, or 50 μM 24 and 48 h NCT-503 significantly inhibited HCC tumor growth in vitro. PMC7541473
Normal human lung fibroblasts (NHLFs) 30 µM 24 hours Treatment with NCT-503 resulted in a dose-dependent decrease in the induction of collagen protein after TGF-β stimulation. PMC5946329
NIH-3T3 cells 30 µM 24 hours NCT-503 treatment reduced TGF-β-induced collagen protein accumulation. PMC5946329
BE(2)-C cells 10 µM 48 hours To assess the impact of NCT-503 on cellular metabolism, results showed that NCT-503 significantly reduced synthesis of glucose-derived citrate and increased the conversion of glucose-derived carbons into malate. PMC8253182
SH-EP cells 10 µM 48 hours To assess the impact of NCT-503 on cellular metabolism, results showed that NCT-503 significantly reduced synthesis of glucose-derived citrate and increased the conversion of glucose-derived carbons into malate. PMC8253182
Kelly cells 10 µM 96 hours To assess the impact of NCT-503 on cell proliferation, results showed that NCT-503 significantly reduced cell viability. PMC8253182
SK-N-AS cells 10 µM 96 hours To assess the impact of NCT-503 on cell proliferation, results showed that NCT-503 significantly reduced cell viability. PMC8253182

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice nude mice Intraperitoneal injection 40 mg/kg daily administration NCT-503 and Sorafenib combination therapy effectively abolished HCC growth. PMC6794322
C57BL/6 and BALB/cFox1nu mice HCC tumors Intraperitoneal injection 40 mg/kg Daily for 14 days NCT-503 combined with Physcion significantly reduced HCC growth. PMC7541473
Mice TC32 xenograft model Intraperitoneal injection 75 mg/kg five days per week for approximately 3 weeks Single-agent NCT-503 significantly inhibited tumor growth, and the combination with GNE-618 completely inhibited tumor growth PMC7335326
Mice bleomycin-induced lung fibrosis model Intraperitoneal injection 40 mg/kg daily for 14 days NCT-503 treatment significantly reduced bleomycin-induced lung fibrosis. PMC5946329
C57BL/KalwRij mice 5T33MM mouse model intraperitoneally (IP) 40 mg/kg 6 times per week for 18 days Evaluate the therapeutic effect of NCT-503 alone or in combination with bortezomib, results showed combination treatment had a therapeutic advantage. PMC7784327

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.24mL

12.24mL

2.45mL

1.22mL

24.48mL

4.90mL

2.45mL

References

 

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