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- CAS号：
137281-23-3
- 规格：
1mLx10mM(inDMSO)/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥148.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥160.0 |
| 规格： | 25mg | 产品价格： | ￥333.0 |
| 规格： | 50mg | 产品价格： | ￥505.0 |
| 规格： | 100mg | 产品价格： | ￥789.0 |
| 规格： | 200mg | 产品价格： | ￥1224.0 |
| 规格： | 500mg | 产品价格： | ￥2064.0 |
Product Introduction
Bioactivity
| 名称 | Pemetrexed |
| 描述 | Pemetrexed (LY-231514 Disodium Hydrate), a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS). |
| 细胞实验 | Pemetrexed is dissolved in DMSO and stored, and then diluted with cell culture medium before use[1]. Dose-response curves are generated to determine the concentration required for 50% inhibition of growth (IC50). Pemetrexed is dissolved initially in DMSO at a concentration of 4 mg/mL and further diluted with cell culture medium to the desired concentration. CCRF-CEM leukemia cells in complete medium are added to 24-well Cluster plates at a final concentration of 4.8×l04 cells/well in a total volume of 2 mL. Test compounds at various concentrations are added to duplicate wells so that the final volume of DMSO is 0.5%. The plates are incubated for 72 h at 37°C in an atmosphere of 5% CO2 in air. At the end of the incubation, cell numbers are determined on a ZBI Coulter counter. Control wells usually contain 4×105 to 6×105 cells at the end of the incubation. For several studies, IC50s are determined for each compound in the presence of either 300 μM AICA, 5 μM thymidine, 100 μM hypoxanthine, or combination of 5 μM hymidine plus 100 μM hypoxanthine[1]. |
| 激酶实验 | AICARFT inhibition assays are carried out at room temperature by monitoring the formation of [6S]-5,6,7,8-tetrahydrofolate from 10-formyl-[6R,S]-5,6,7,8-tetrahydrofolate at A298. All solutions are purged with N2 gas prior to use. The reaction solution contains 33 mM Tris-Cl, pH 7.4, 25 mM KCl, 5 mM 2-Mercaptoethanol, 0.05 mM AICA ribonucleotide, and 16 nM (2 milliunits/mL) of AICARFT. 10-Formyl-[6R,S]-5,6,7,8-tetrahydrofolate concentrations of 0.037, 0.074, and 0.145 mM are used (0.61, 1.23, and 2.45 times its Km value, respectively). LY231514 is tested as an inhibitor at 0.08-0.8 mM (four concentrations). When the tri- and pentaglutamates of LY231514 are used as inhibitors, the concentrations are 0.0005-0.009 mM (eight concentrations). Enzyme assays are initiated by the addition of enzyme. Data is analyzed using the ENZFITTER program for competitive inhibition. |
| 体外活性 | Pemetrexed (LY231514) disodium is a novel classical antifolate, the antitumor activity of which may result from simultaneous and multipie inhibition of several key folate-requiring enzymes via its polyglutamated metabolites. Pemetrexed (LY231514) is one of the best substrates that is known for the enzyme FPGS (Km=1.6 μM and Vmax/Km=621). It is likely that polyglutamation and the polyglutamated metabolites of LY231514 play profound roles in determining both the selectivity and the antitumor activity of this novel agent. Whereas LY23l5l4 only moderately inhibits TS (Ki=340 nM, recombinant mouse), the pentaglutamate of LY23l5l4 is 100-fold more potent (Ki=3.4 nM), making LY231514 one of the most potent folate-based TS inhibitors[1]. |
| 体内活性 | The group of mice treated with PC61 plus Pemetrexed indicates statistically longer survival than other groups. In survival analysis, significantly better survival is observed in the group of mice treated with PC61 plus Pemetrexed compare with those treated with PC61 alone, rat IgG plus Pemetrexed, or untreated[2]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.68 mM), Sonication is recommended. DMSO : 35 mg/mL (81.89 mM), Sonication is recommended. |
| 关键字 | Thymidylate synthase | RNASynthesis | RNA Synthesis | LY-231514 Disodium Hydrate | GARFT | DNASynthesis | DNA Synthesis | DHFR | Autophagy | Antifolate |
| 相关产品 | Urea | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Thymidine | Paeonol |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | EMA Approved Drug Library | Failed Clinical Trials Compound Library | Anti-Aging Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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培美曲塞【137281-23-3】
￥148 - 2064
