NCT-503-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENCT-503Cat. No.: HY-101966CAS No.: 1916571-90-8分式: CHFNS分量: 408.48作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (122.41 mM; Need ultrasonic)Mass Solvent1 mg

2、 5 mg 10 mg Concentration制备储备液1 mM 2.4481 mL 12.2405 mL 24.4810 mL5 mM 0.4896 mL 2.4481 mL 4.8962 mL10 mM 0.2448 mL 1.2241 mL 2.4481 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液

3、中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.12 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.12 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 NCT-503磷酸油酸脱氢酶

4、(PHGDH) 抑制剂，IC50 值为2.5 M。IC50 & Target IC50: 2.5 M (PHGDH) 1体外研究 Human phosphoglycerate dehydrogenase (PHGDH) catalyzes the first, rate-limiting step in the canonicalglucose-derived serine synthesis pathway. NCT-503, a PHGDH inhibitor, inhibits serine synthesis from 3-phosphoglycerate in cells (IC50

5、=2.5 M). NCT-503 is inactive against a panel of other dehydrogenases andshows 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 withrespect to both 3-PG and NAD+. NC

6、T-503 has EC50s of 816 M 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 lines1.体内研究 NCT-503 exhibits favorable absorption, distribution, metabolism and excretion (ADME) properties. NCT-503has good exposure, ha

7、lf-life (2.5 hr) and Cmax (20 M in plasma) following intraperitoneal administration withsignificant 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

8、 xenografts 1.PROTOCOLCell Assay 1 MDA-MB-468, BT-20, MT-3 cells are seeded in white 96-well plates allowed to attach for 24 hours. Cells aretreated with NCT-503 for four days. Cell viability is assessed with Cell Titer-Glo and luminescence measuredwith a plate reader 1.MCE has not independently con

9、firmed the accuracy of these methods. They are for reference only.Animal Mice: Chronic catheters are surgically implanted into the jugular veins of normal or tumor bearing animals 3-4Administration 1 days prior to infusions. Following administration of either vehicle or NCT-503 at 30 mg/kg, a consta

10、nt infusionof U-13C-glucose (30 mg/kg/min) is administered for a 3-hour duration. Animals are terminally anesthetizedwith sodium pentobarbital and all tissues are fully harvested in less than 5 minutes to preserve the metabolicstate. Tumors and adjacent lung tissue are carefully dissected and rapidl

11、y frozen for analysis 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Mol Cell. 2019 Aug. Nat Commun. 2019 Jun 20;10(1):2701.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Pacold ME, et al. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol. 20162/3 Master of Small Molecules 您边的抑制剂师www.MedChemEJun;12(6):452-8.McePdfHeightCaution: Product h