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- Solarbio
- 北京
- IP01201
- 2025年07月23日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Stroe at -20℃，6 months.
- 保质期：
Stroe at -20℃，6 months.
- 英文名：
Pemetrexed(10mM in DMSO,Sterile）
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
137281-23-3
- 规格：
0.1ml/0.3ml/0.5ml/1.5ml/1ml
| 规格： | 0.1ml | 产品价格： | ￥360.0 |
|---|---|---|---|
| 规格： | 0.3ml | 产品价格： | ￥540.0 |
| 规格： | 0.5ml | 产品价格： | ￥720.0 |
| 规格： | 1.5ml | 产品价格： | ￥1170.0 |
| 规格： | 1ml | 产品价格： | ￥900.0 |
| 基本信息 | |
| CAS | No.137281-23-3 |
| 中文名称 | 培美曲塞酸(10mM in DMSO,无菌） |
| 英文名称 | Pemetrexed(10mM in DMSO,Sterile） |
| 分子式 | C20H21N5O6 |
| 分子量 | 427.41 |
| 溶解性 | 请根据自己的实验要求使用。 |
| 外观(性状) | 无菌溶液 |
| 储存条件 | Stroe at -20℃，6 months. |
| 靶点 | Antifolate;DHFR;GARFT |
| 通路 | Cell Cycle;DNA Damage/DNA Repair;Metabolic Enzyme&Protease |
| 背景说明 | Pemetrexed是一种叶酸拮抗剂，可结合并抑制胸苷酸合成酶 (TS)，二氢叶酸还原酶 (DHFR) 和甘氨酰胺核苷酸甲酰转移酶 (GARFT)。 |
| 生物活性 | Pemetrexed (LY231514) is an antifolate， the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3， 7.2， and 65 nM for inhibits thymidylate synthase (TS)， dihydrofolate reductase (DHFR)， and glycinamide ribonucleotide formyltransferase (GARFT)， respectively.[1-2] |
| IC50 | Ki: 1.3 nM (TS)， 7.2 nM (DHFR)， 65 nM (GARFT)[1] |
| In Vitro | 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]. |
| 细胞实验 | 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[2]. |
| 细胞实验 | 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 4.8×104 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]. |
| 动物实验 | Mice[2] Female CBA mice and female NOD/SCID mice (NOD.CB17-Prkdcscid) at 6-8 wk of age are used. Premetrexed (100 mg/kg) is given i.p. from days 4-8 (5 consecutive d) to tumor-bearing mice to explore the synergistic effect when combined with anti-CD25 Ab or IgG control. The dose and schedule used for Pemetrexed in the current study is determined based on previous studies in mice. |
| 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.[1-2] |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
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于宿主细胞编码的某些酶和蛋白质，如离开宿主细胞则不能存活,而宿主即使没有它们也可以正常存活。质粒的存在使宿主具有一些额外的特性,如对抗生素的抗性等。F质粒(又称F因子或性质粒)、R质粒(抗药性因子)和Col质粒(产大肠杆菌素因子)等都是常见的天然质粒。 质粒在细胞内的复制一般有两种类型:紧密控制型(Stringent control)和松驰控制型(Relaxed control)。前者只在细胞周期的一定阶段进行复制,当染色体不复制时,它也不能复制,通常每个细胞内只含有1个或几个质粒分子
于宿主细胞编码的某些酶和蛋白质，如离开宿主细胞则不能存活,而宿主即使没有它们也可以正常存活。质粒的存在使宿主具有一些额外的特性,如对抗生素的抗性等。F质粒(又称F因子或性质粒)、R质粒(抗药性因子)和Col质粒(产大肠杆菌素因子)等都是常见的天然质粒。 质粒在细胞内的复制一般有两种类型:紧密控制型(Stringent control)和松驰控制型(Relaxed control)。前者只在细胞周期的一定阶段进行复制,当染色体不复制时,它也不能复制,通常每个细胞内只含有1个或几个质粒分子
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IP01201 培美曲塞酸(10mM in DMSO,无菌） 细胞周期 索莱宝
￥360 - 1170
