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  • 培美曲塞二钠盐|T0189L

培美曲塞二钠盐|T0189L

Pemetrexed disodium
150399-23-8
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上海 更新日期：2024-09-14

TargetMol中国（陶术生物）

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邮箱：marketing@targetmol.com

产品详情:

中文名称：
培美曲塞二钠盐
英文名称：
Pemetrexed disodium
CAS号：
150399-23-8
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.92%
产品类别：
抑制剂
货号：
T0189L

Product Introduction

Bioactivity

名称Pemetrexed disodium
描述Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma. Pemetrexed disodium therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liver injury.
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)
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.
体外活性Pemetrexed作用于人类H460非小细胞肺癌移植瘤,抑制肿瘤生长.Pemetrexed和紫杉醇联用,更大程度推迟H460肿瘤生长.
体内活性研究显示顺铂和Pemetrexed联用作用于感染腺病毒表达SOCS-1载体的MPM细胞,通过抑制细胞增殖侵入和诱导凋亡而产生抗癌作用。Pemetrexed有效作用于CCRF-CEM白血病,GC3/C1结肠癌和HCT-8 回盲肠癌细胞,具有抗增殖活性,IC50分别为25 nM,34 nM 和220 nM。Pemetrexed有效抑制胸苷酸合酶,Ki为1.3 nM,也明显抑制其他关键叶酸酶,包括二氢叶酸还原酶和甘氨酰胺核苷酸转甲酰酶,Ki分别为7.2 nM和 65 nM。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 4.71 mg/mL (10 mM)
关键字Apoptosis | Autophagy | LY 231514 | Antifolate | LY231514 | inhibit | Inhibitor | Pemetrexed disodium
相关产品Guanidine hydrochloride | Naringin | Hydroxychloroquine | Stavudine | Thymidine | Paeonol | Sodium 4-phenylbutyrate
相关库抑制剂库 | 抗癌活性化合物库 | 抗癌上市药物库 | 经典已知活性库 | EMA 上市药物库 | 抗衰老化合物库 | FDA 上市药物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库
LY-231514|||LY231514 disodium|||培美曲塞二钠|||Pemetrexed|||培美曲塞二钠盐

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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