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NCT-503
CAS No. : 1916571-90-8
MCE 国际站:NCT-503
产品活性:NCT-503磷酸甘油酸脱氢酶 (PHGDH) 抑制剂,IC50 值为2.5 µM。
研究领域:Metabolic Enzyme/Protease
作用靶点:Phosphoglycerate Dehydrogenase (PHGDH)
In Vitro: NCT-503, a PHGDH inhibitor, inhibits serine synthesis from 3-phosphoglycerate in cells (IC50=2.5 μM). NCT-503 is inactive against a panel of other dehydrogenases and shows 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 with respect to both 3-PG and NAD+. NCT-503 has EC50s of 8–16 μM 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 lines.
In Vivo: NCT-503 exhibits favorable absorption, distribution, metabolism and excretion (ADME) properties. NCT-503 has good exposure, half-life (2.5 hr) and Cmax (20 μM in plasma) following intraperitoneal administration with significant 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 xenografts.
相关产品:Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Targeted Diversity Library | Heterocyclic Compound Library | CBR-5884 | BI-4916 | NCT-502 | PHGDH-inactive | PKUMDL-WQ-2101 | PHGDH-IN-3 | PKUMDL-WQ-2201 | PHGDH-IN-2
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文献和实验miRcute 血清/血浆 miRNA 提取分离试剂盒 (DP503) 操作指南
以下操作按照天根产品 DP503 miRcute 血清/血浆 miRNA 提取分离试剂盒的说明书进行,所有反应现象仅适用于该产品及本文所标明的样本量。如使用其它操作流程或产品,样本量不同可能现象与本文有所差异。实验准备:1. 血清/血浆样本2. 无水乙醇,氯仿3. 移液器及配套RNase-Free无菌枪头(200 μl ,1 ml); 1.5 ml,2.0 ml 离心管(RNase-free)4. 涡旋振荡器,台式低温离心机,金属浴/水浴实验准备-试剂盒准备:第一次使用前应在去蛋白液RD、漂洗
血氨及数字连接试验(NCT)。结果:治疗组治疗后血氨36 μmol.L-1±12 μmol.L-1,NCT 52 s±23 s;对照组血氨52 μmol.L-1±18 μmol.L-1,NCT 81 s±26 s(P<0.01)。结论:乳果糖治疗SHE有效、方便、安全。 [中图分类号] R975.3;R575.2 [文献标识码] B [文章编号] 1007-7669(2000)06-0523-02 亚临床肝性脑病(subclinical hepatic
患者加入了一项附加的免疫检查点抑制剂试验,其中5名患者出现反应。Kim等人最近的一项研究。证明恩替司他和5-氮胞苷与PD-1和CTLA-4(细胞毒性T淋巴细胞相关抗原4;免疫抑制剂)的组合治愈了转移性乳腺癌模型中80%的小鼠。事实上,单用HDAC抑制结合PD-1和CTLA-4抗体可100%抑制原发性肿瘤和转移(结直肠和乳腺小鼠模型)。表观遗传学机制涉及抑制髓样细胞。目前,一项二期临床试验正在肺癌(NCT 01928576)中进行,该试验在nivolumab之前单独使用氮胞苷或与环磷酰胺联合
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