NCT-503
- CAS No.
- 1916571-90-8
- Chemical Name:
- NCT-503
- Synonyms
- NCT-503;CS-2612;NCT 503;NCT503;NCT-503 >=98% (HPLC);NCT-503, 10 mM in DMSO;NCT-503; NCT 503; NCT503.;inhibit,NCT-503,NCT503,Inhibitor;N-(4,6-Dimethylpyridin-2-yl)-4-(4-(trifluoromethyl)benzyl)piperazine-1-carbothioamide;1-Piperazinecarbothioamide, N-(4,6-dimethyl-2-pyridinyl)-4-[[4-(trifluoromethyl)phenyl]methyl]-;9-(6-aminopyridin-3-yl)-1-(4-fluoro-3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one
- CBNumber:
- CB83159381
- Molecular Formula:
- C20H23F3N4S
- Molecular Weight:
- 408.48
- MDL Number:
- MFCD30343875
- MOL File:
- 1916571-90-8.mol
- MSDS File:
- SDS
| Boiling point | 474.3±55.0 °C(Predicted) |
|---|---|
| Density | 1.306±0.06 g/cm3(Predicted) |
| storage temp. | 2-8°C |
| solubility | ≥40.9 mg/mL in DMSO; insoluble in H2O; ≥20.33 mg/mL in EtOH |
| form | powder |
| pka | 12.99±0.20(Predicted) |
| color | white to beige |
| InChI | InChI=1S/C20H23F3N4S/c1-14-11-15(2)24-18(12-14)25-19(28)27-9-7-26(8-10-27)13-16-3-5-17(6-4-16)20(21,22)23/h3-6,11-12H,7-10,13H2,1-2H3,(H,24,25,28) |
| InChIKey | PJNSZIQUFLWRLH-UHFFFAOYSA-N |
| SMILES | N1(C(NC2=NC(C)=CC(C)=C2)=S)CCN(CC2=CC=C(C(F)(F)F)C=C2)CC1 |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
NCT-503 price More Price(14)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML1659 | NCT-503 ≥98% (HPLC) | 1916571-90-8 | 5MG | $105.45 | 2025-07-31 | Buy |
| Sigma-Aldrich | SML1659 | NCT-503 ≥98% (HPLC) | 1916571-90-8 | 25MG | $447 | 2025-07-31 | Buy |
| Cayman Chemical | 19718 | NCT-503 ≥98% | 1916571-90-8 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 19718 | NCT-503 ≥98% | 1916571-90-8 | 5mg | $86 | 2024-03-01 | Buy |
| Cayman Chemical | 19718 | NCT-503 ≥98% | 1916571-90-8 | 10mg | $153 | 2024-03-01 | Buy |
NCT-503 Chemical Properties,Uses,Production
Description
NCT-503 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells with an IC50 value of 2.5 μM. It has been shown to reduce the production of glucose-derived serine in cells and to suppress the growth of PHGDH-dependent MDA-MB-468 cancer cells both in vitro and in mice bearing orthotopic xenograft tumors.
Uses
NCT-503 is a novel inhibitor of human Phosphoglycerate Dehydrogenase (PHGDH).
Biochem/physiol Actions
NCT-503 is an inhibitor of phosphoglycerate dehydrogenase (PHGDH), which catalyzes the first, rate-limiting step of glucose-derived serine synthesis. NCT-503 reduced glucose-derived serine production and suppressed the growth of both PHGDH-dependent cancer cells in culture and in xenograft tumors, and caused G1/S cell cycle arrest in MDA-MB-468 cells. NCT-503 reduced the incorporation of one-carbon units from glucose-derived and exogenous serine into nucleotides, which may contribute to its anticancer activity. NCT-503 had an IC50 value of 2.5 μM for PHGDH and was inactive against a panel of other dehydrogenases and minimal cross-reactivity in a panel of 168 G-protein-coupled receptors (GPCRs). NCT-503 was found to be noncompetitive with respect to both 3-PG and NAD+, and exhibit good stability (>98% after 48 hrs in assay buffer) and aqueous solubility.
in vitro
nct-503 was identified as an inhibitor of phgdh and was found to be inactive against a panel of other dehydrogenases and showed minimal cross-reactivity in a panel of g-protein-coupled receptors. in addition, treatment of three phgdh-independent cell lines and five phgdhdependent cell lines with nct-503 demonstrated that nct-503 had ec50 values of 8–16 μm for the phgdh-dependent cell lines, and no toxicity toward other phgdh-independent cell lines [1].
in vivo
to evaluate nct-503 in-vivo activity, nod.scid mice bearing mda-mb-231 and mda-mb-468 orthotopic xenografts were treated with vehicle or nct-503. results showed that nct-503 treatment reduced the growth and weight of phgdh-dependent xenografts but did not affect those of phgdh-independent xenografts. importantly, mice treated with nct-503 did not lose weight during the 24-d treatment in spite of the potential systemic toxicities of inhibiting serine biosynthesis [1].
IC 50
2.5 μm for inhibiting serine synthesis from 3-phosphoglycerate in cells
References
[1] pacold, m. e.,brimacombe, k.r.,chan, s.h., et al. a phgdh inhibitor reveals coordination of serine synthesis and one-carbon unit fate. nature chemical biology 12(6), 452-458 (2016).
NCT-503 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 +8618813727289 | contact@trustwe.com | China | 5744 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32432 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30229 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49734 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39031 | 58 |
