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Pemetrexed

产品编号 T0189 CAS 137281-23-3

别名: Pemetrexed acid, 培美曲塞, LY231514, 培美曲唑, LY-231514 Disodium Hydrate

Pemetrexed (LY-231514 Disodium Hydrate) acid 是一种鸟嘌呤衍生的抗肿瘤药物，可结合并抑制胸苷酸合酶、二氢叶酸还原酶和甘氨酰胺核苷酸甲酰转移酶的 Ki 分别为 1.3 nM、7.2 nM 和 65 nM。

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Pemetrexed, CAS 137281-23-3

规格	价格/CNY	货期
10 mg	￥ 180	现货
25 mg	￥ 397	现货
50 mg	￥ 632	现货
100 mg	￥ 987	现货
200 mg	￥ 1,530	现货
500 mg	￥ 2,580	现货
1 mL * 10 mM (in DMSO)	￥ 638	现货

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其他形式的 Pemetrexed:

Pemetrexed disodium
现货
Pemetrexed disodium hemipenta hydrate
现货
Pemetrexed tromethamine
询价
Pemetrexed disodium heptahydrate
询价

选择批次

纯度: 100%

纯度: 99.96%

纯度: 99.92%

纯度: 99.78%

纯度: 99.58%

纯度: 98.1%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Pemetrexed (LY-231514 Disodium Hydrate), a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).
靶点活性	TS:1.3 nM(ki), DHFR:7.2 nM(ki), GARFT:65 nM(ki)
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].
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.
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].

别名	Pemetrexed acid, 培美曲塞, LY231514, 培美曲唑, LY-231514 Disodium Hydrate
分子量	427.41
分子式	C20H21N5O6
CAS No.	137281-23-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (233.97 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3397 mL	11.6984 mL	23.3967 mL	58.4918 mL
	5 mM	0.4679 mL	2.3397 mL	4.6793 mL	11.6984 mL
	10 mM	0.234 mL	1.1698 mL	2.3397 mL	5.8492 mL
	20 mM	0.117 mL	0.5849 mL	1.1698 mL	2.9246 mL
	50 mM	0.0468 mL	0.234 mL	0.4679 mL	1.1698 mL
	100 mM	0.0234 mL	0.117 mL	0.234 mL	0.5849 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Shih C, et al. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Res. 1997 Mar 15;57(6):1116-23. 2. Anraku M, et al. Synergistic antitumor effects of regulatory T cell blockade combined with pemetrexed in murine malignantmesothelioma. J Immunol. 2010 Jul 15;185(2):956-66.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

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。

Keywords

Pemetrexed 137281-23-3 Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism DHFR DNA/RNA Synthesis Antifolate inhibit LY 231514 Pemetrexed acid 培美曲塞 LY-231514 LY231514 Inhibitor 培美曲唑 LY-231514 Disodium Hydrate inhibitor

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Pemetrexed

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords