≥40.9 mg/mL in DMSO; insoluble in H2O; ≥20.33 mg/mL in EtOH
물리적 상태
가루
산도 계수 (pKa)
12.99±0.20(Predicted)
색상
흰색에서 베이지색
안전
위험 및 안전 성명
위험 및 사전주의 사항 (GHS)
그림문자(GHS):
신호 어:
Warning
유해·위험 문구:
암호
유해·위험 문구
위험 등급
범주
신호 어
그림 문자
P- 코드
H315
피부에 자극을 일으킴
피부부식성 또는 자극성물질
구분 2
경고
P264, P280, P302+P352, P321,P332+P313, P362
예방조치문구:
P280
보호장갑/보호의/보안경/안면보호구를 착용하시오.
NFPA 704
0
1
0
NCT-503 C화학적 특성, 용도, 생산
개요
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.
용도
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.
