Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NCT-503 是一种磷酸甘油酸脱氢酶 (PHGDH) 抑制剂,其IC50=2.5 µM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 237 | 现货 | ||
2 mg | ¥ 336 | 现货 | ||
5 mg | ¥ 543 | 现货 | ||
10 mg | ¥ 828 | 现货 | ||
25 mg | ¥ 1,620 | 现货 | ||
50 mg | ¥ 2,570 | 现货 | ||
100 mg | ¥ 3,950 | 现货 | ||
200 mg | ¥ 5,470 | 现货 | ||
500 mg | ¥ 8,390 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 589 | 现货 |
产品描述 | NCT-503 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells. |
靶点活性 | PHGDH:2.5 μM |
体外活性 | NCT-503 has reasonable aqueous solubility, and exhibits favorable absorption, distribution, metabolism and excretion (ADME) properties[1]. NCT-503 selectively blocks glucose-derived serine synthesis but at the same time triggers SHMT1-dependent one-carbon unit wasting to synthesize serine from glycine. This futile cycle depletes the cell of nucleotides and leads to cell cycle arrest |
体内活性 | NCT-503 has good exposure (AUClast=14,700 hr*ng/mL), half-life (2.5 hr) and Cmax (~20 μM in plasma) following intraperitoneal administration with significant partitioning into the liver and brain. PHGDH inhibition by NCT-503 selectively increases necrosis in MDA-MB-468 xenografts, but not in MDA-MB-231 xenografts. It also 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 xenografts |
动物实验 | Animal Models: NOD.SCID mice bearing MDA-MB-231 and MDA-MB-468 orthotropic xenograftsFormulation: 5% ethanol, 35% PEG 300, and 60% of an aqueous 30% hydroxypropyl-β-cyclodextrin solutionDosages: 40 mg/kgAdministration: i.p.(Only for Reference) |
别名 | NCT 503 |
分子量 | 408.48 |
分子式 | C20H23F3N4S |
CAS No. | 1916571-90-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 75 mg/mL (183.6 mM)
DMSO: 75 mg/mL (183.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.4481 mL | 12.2405 mL | 24.481 mL | 61.2025 mL |
5 mM | 0.4896 mL | 2.4481 mL | 4.8962 mL | 12.2405 mL | |
10 mM | 0.2448 mL | 1.2241 mL | 2.4481 mL | 6.1203 mL | |
20 mM | 0.1224 mL | 0.612 mL | 1.2241 mL | 3.0601 mL | |
50 mM | 0.049 mL | 0.2448 mL | 0.4896 mL | 1.2241 mL | |
100 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.612 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
NCT-503 1916571-90-8 Angiogenesis Metabolism Tyrosine Kinase/Adaptors FLT Dehydrogenase TAM Receptor inhibit Inhibitor NCT503 NCT 503 inhibitor