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培美曲塞  ≥98%

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包装规格：250mg 1g 5g in glass bottle
溶解性：溶于DMSO（≥ 100 mg/mL）
产品描述：基本信息 产品编号：P10865 产品名称：Pemetrexed CAS: 137281-23-3   储存条件 粉末 -20℃ 四年     分子式： C20H21N5O6 溶于液体 -80℃ 六个月 分子量 427.41 -20℃ 一个月 化学名：  (S)-2-(4-(2-(2-Amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido)pentanedioic acid   Solubility (25°C)   体外 DMSO 200mg/mL (467.93mM; Need ultrasonic) Ethanol   Water   体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3397mL 11.6984mL 23.3967mL 5mM 0.4679mL 2.3397mL 4.6793mL 10mM 0.2340mL 1.1698mL 2.3397mL   生物活性 产品描述 一种叶酸拮抗剂 (antifolate)。Pemetrexed (LY231514) 抑制胸苷酸合成酶 (TS)，二氢叶酸还原酶 (DHFR) 和甘氨酰胺核苷酸甲酰转移酶 (GARFT)，Ki 分别为 1.3nM，7.2nM 和 65nM。 靶点/IC50 Ki: 1.3nM (TS), 7.2nM (DHFR), 65nM (GARFT)   体外研究 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=1.6μM 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=340nM,recombinant mouse), the pentaglutamate of LY23l5l4 is 100-fold more potent (Ki=3.4nM), making LY231514 one of the most potent folate-based TS inhibitors.   体内研究 The group of mice treated with PC61 plus Pemetrexed demonstrates statistically longer survival than other groups. In a 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 no treatment.   推荐实验方法(仅供参考) 激酶实验： Kinase Assay 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 33mM Tris-Cl, pH 7.4, 25mM KCl, 5mM 2-Mercaptoethanol, 0.05mM AICA ribonucleotide, and 16nM (2 milliunits/mL) of AICARFT. 10-Formyl-[6R,S]-5,6,7,8-tetrahydrofolate concentrations of 0.037, 0.074, and 0.145mM are used (0.61, 1.23, and 2.45 times its Km value, respectively). LY231514 is tested as an inhibitor at 0.08-0.8mM (four concentrations). When the tri- and pentaglutamates of LY231514 are used as inhibitors, the concentrations are 0.0005-0.009mM (eight concentrations). Enzyme assays are initiated by the addition of enzyme. Data is analyzed using the ENZFITTER program for competitive inhibition.   细胞实验:   Cell Assay 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 4mg/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 4.8×104 cells/well in a total volume of 2mL. 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 300μM AICA, 5μM thymidine, 100μM hypoxanthine, or combination of 5μM hymidine plus 100μM hypoxanthine .   动物实验:   Animal Administration Mice Female CBA mice and female NOD/SCID mice (NOD.CB17-Prkdcscid) at 6-8 wk of age are used. Premetrexed (100mg/kg) is given i.p. from days 4-8 (5 consecutive d) to tumor-bearing mice to explore the synergistic effect when combined with antiCD25 Ab or IgG control. The dose and schedule used for Pemetrexed in the current study is determined based on previous studies in mice.
保存条件：-20℃

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