NCT-503-DataSheet-生命科學(xué)試劑-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作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (122.41 mM; Need ultrasonic)Mass Solvent1 mg

2、 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液

3、中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.12 mM); Suspended solution; Need ultrasonic2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.12 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 NCT-503磷酸油酸脫氫酶

4、(PHGDH) 抑制劑，IC50 值為2.5 M。IC50 & Target IC50: 2.5 M (PHGDH) 1體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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 您邊的抑制劑師www.MedChemEJun;12(6):452-8.McePdfHeightCaution: Product h