ChemicalBook >> CAS DataBase List >>NCT-503

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; 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
Last updated:2023-06-08 09:01:58

NCT-503 Properties

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

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315
Precautionary statements  P280
NFPA 704
0
1 0

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 2023-06-20 Buy
Sigma-Aldrich SML1659 NCT-503 ≥98% (HPLC) 1916571-90-8 25MG $424 2023-06-20 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
Product number Packaging Price Buy
SML1659 5MG $105 Buy
SML1659 25MG $424 Buy
19718 1mg $32 Buy
19718 5mg $86 Buy
19718 10mg $153 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

Global( 76)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
BOC Sciences
+1-631-485-4226 inquiry@bocsci.com United States 19553 58
SHANGHAI T&W PHARMACEUTICAL CO., LTD.
+86-021-61551413 +8618813727289 contact@trustwe.com China 5739 58
Career Henan Chemica Co
+86-0371-86658258 15093356674; laboratory@coreychem.com China 30255 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6313 58
InvivoChem
+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6393 58
Hangzhou MolCore BioPharmatech Co.,Ltd.
+86-057181025280; +8617767106207 sales@molcore.com China 49739 58
Nantong HI-FUTURE Biology Co., Ltd.
+undefined18051384581 sales@chemhifuture.com China 3136 58
TargetMol Chemicals Inc.
+1-781-999-5354 support@targetmol.com United States 19973 58
Wuhan Topule Biopharmaceutical Co., Ltd
+8618327326525 masar@topule.com China 8475 58

NCT-503 Spectrum

NCT-503 9-(6-aminopyridin-3-yl)-1-(4-fluoro-3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one NCT 503;NCT503 CS-2612 NCT-503; NCT 503; NCT503. 1-Piperazinecarbothioamide, N-(4,6-dimethyl-2-pyridinyl)-4-[[4-(trifluoromethyl)phenyl]methyl]- NCT-503 >=98% (HPLC) inhibit,NCT-503,NCT503,Inhibitor N-(4,6-Dimethylpyridin-2-yl)-4-(4-(trifluoromethyl)benzyl)piperazine-1-carbothioamide 1916571-90-8 C20H23F3N4S