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Pemetrexed disodium hemipenta hydrate

产品编号 T6226 CAS 357166-30-4

别名: 培美曲塞二钠一水合物, Pemetrexed Disodium Hydrate, LY-231514 Disodium Hydrate, Pemetrexed sodium hydrate, 培美曲塞二钠水合物

Pemetrexed disodium hemipenta hydrate (LY-231514 Disodium Hydrate) 是一种叶酸拮抗剂。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 1.3 nM，7.2 nM 和 65 nM。

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Pemetrexed disodium hemipenta hydrate Chemical Structure

Pemetrexed disodium hemipenta hydrate, CAS 357166-30-4

规格	价格/CNY	货期
25 mg	￥ 298	现货
50 mg	￥ 428	现货
100 mg	￥ 622	现货
200 mg	￥ 939	现货
500 mg	￥ 1,720	现货

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其他形式的 Pemetrexed disodium hemipenta hydrate:

选择批次

纯度: 99.16%

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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 disodium hemipenta hydrate (LY-231514 Disodium Hydrate) is a new-type antifolate and antimetabolite for TS, DHFR, and GARFT. The Ki of Pemetrexed Disodium Hydrate for TS, DHFR and GARFT is 1.3 nM, 7.2 nM and 65 nM, respectively.
靶点活性	GARFT:65 nM(Ki), TS:1.3 nM(Ki), DHFR:7.2 nM(Ki)
体外活性	在人H460非小细胞肺癌异种移植模型中,Pemetrexed disodium能够抑制肿瘤生长.
体内活性	\在CCRF-CEM白血病,GC3/C1结肠癌,和HCT-8回盲部结肠癌细胞中,Pemetrexed disodiumIC50分别为25 nM,34 nM和220 nM,表现出抗肿瘤活性。
激酶实验	Enzyme Assays and Methods.: TS activity is assayed using a spectrophotometric method,which involved monitoring the increase in absorbance at 340 nm resulting from formation of the product,7,8-dihydrofolate.The assay buffer contains 50 mM N-tris[hydroxymethyljmethyl-2-aminoethanesulfonic acid,25 mM MgC12,6.5 mM formaldehyde,1 mM EDTA,and 75 mM 2-mercaptoethanol,pH 7.4.The concentrations of deoxyuridylate monophosphate,6R-MTHF,and hIS are 100 μM,30 μM and 30 nM (1.7 milliunits/mL),respectively.At the 6R-MTHF concentration,an uninhibited reaction and six concentrations of inhibitor are assayed.Ki app values are determined by fitting the data to the Morrison equation using nonlinear regression analysis with the aid of the program ENZFITTER.Ki values are calculated using the equation: Ki app= Ki(1 + [S]/Km),where [S] is equal to 30 μM and Km is equal to 3 μM.DHFR activity is assayed spectrophotometrically by monitoring the dis appearance of the substrates NADPH and 7,8-dihydrofolate at 340 nm.The reaction takes place at 25°C in 0.5 mL of 50 mM potassium phosphate buffer,which contains 150 mM KC1 and 10 nM 2-mercaptoethanol,pH 7.5,and 14 nM (0.34 milliunitlmL) DHFR.The NADPH concentration is 10 μM and 7,8-dihydrofolate is varied at 5,10,or 15 μM.At each 7,8-dihydrofolate concentration,an uninhibited reaction and seven concentrations of inhibitor are assayed.The ENZFITI'ER microcomputer program is used to obtain Ki app values by fitting the data to the Morrison equation by nonlinear regression analysis.Ki app= Ki(1 + [S]/Km),where [S] is equal to the concentration of 7,8-dihydrofolate used and Km of 7,8-dihydrofolate is equal to 0.15 μM.GARFT activity is assayed spectrophotometrically by monitoring the increase of absorbance resulting from formation of the product 5,8-dideazafolate at 295 nm.The reaction solvent contains 75 mM HEPES,20% glycerol,and 50 mM a-thioglygerol,pH 7.5,at 25°C.
细胞实验	Dose-response curves are generated to determine the concentration required for 50% inhibition of growth (IC50). Pemetrexed disodium 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 in a total volume of 2.0 mL. Pemetrexed disodium at various concentrations are added to duplicate wells so that the final volume of DMSO is 0.5%. The plates are incubated for 72 hour 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. 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. For adherent tumor cells, a modification of the original MTT colorimetric assay is used to measure cell cytotoxicity. The human tumor cells are seeded in 100 μL assay medium/well in 96-well flat-bottomed tissue culture plates. The assay medium contains folic acid-free RPMI 1640 supplemented with 10% FCS and either 2 nM folinic acid or 2.3 μM folic acid as the sole folate source. Well 1A is left blank. Stock solutions of antifolates are prepared in Dulbecco's PBS at 1 mg/mL, and a series of 2-fold dilutions are subsequently made in PBS. Ten-μL aliquots of each concentration are added to triplicate wells. Plates are incubated for 72 hours at 37 °C in a humidified atmosphere of 5% CO2-in-air. MTT is dissolved in PBS at 5 mg/mL, 10 μL of stock MTF solution are added to each well of an assay, and the plates are incubated at 37 °C for 2 additional hours. Following incubation, 100 μL of DMSO are added to each well. After thorough formazan solubilization, the plates are read on a Dynatech MR600 reader, using a test wavelength of 570 nm and a reference wavelength of 630 nm.The IC50 is determined as the concentration of drug required to inhibit cell growth by 50% compared to an untreated controls.(Only for Reference)

别名	培美曲塞二钠一水合物, Pemetrexed Disodium Hydrate, LY-231514 Disodium Hydrate, Pemetrexed sodium hydrate, 培美曲塞二钠水合物
分子量	518.43
分子式	C20H21N5O6·2Na·5/2H2O
CAS No.	357166-30-4

存储

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

溶解度

DMSO: Slightly soluble

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. Cancer Res. 1997, 57(6), 1116-1123. 2. Iwahori K, et al. Int J Cancer. 2012, doi: 10.1002/ijc.27611. 3. Teicher BA, et al. Clin Cancer Res. 2000, 6(3), 12016-1023.

文献引用

1. Bi G, Liang J, Zhao M, et al. MiR-6077 promotes cisplatin/pemetrexed resistance in lung adenocarcinoma by targeting CDKN1A/cell cycle arrest and KEAP1/ferroptosis pathways. Molecular Therapy-Nucleic Acids. 2022 2. Zhao G, Liang J, Shan G, et al.KLF11 regulates lung adenocarcinoma ferroptosis and chemosensitivity by suppressing GPX4.Communications Biology.2023, 6(1): 570.

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

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给药体积

μL

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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+

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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。

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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 disodium hemipenta hydrate 357166-30-4 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism DHFR DNA/RNA Synthesis Antifolate 培美曲塞二钠一水合物 Pemetrexed Disodium Hydrate LY-231514 Disodium Hydrate LY231514 disodium hemipenta inhibit Pemetrexed sodium hydrate Pemetrexed disodium hemipenta Inhibitor 培美曲塞二钠水合物 Pemetrexed sodium Hydrate Pemetrexed disodium hemipenta Hydrate inhibitor

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Pemetrexed disodium hemipenta hydrate

存储

溶解度

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参考文献

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剂量换算

体内实验配液计算器

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