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- 文献和实验
- 技术资料
- 库存：
999
- 英文名：
Pemetrexed Disodium(10mM in Water，Sterile)
- CAS号：
357166-30-4
- 保质期：
Store at -20℃，6 months
- 供应商：
北京索莱宝科技有限公司
- 保存条件：
Store at -20℃，6 months
- 规格：
1ml
| CAS | 357166-30-4 |
| 中文名称 | 培美曲塞二钠水合物(10mM in Water，无菌） |
| 英文名称 | Pemetrexed Disodium(10mM in Water，Sterile) |
| 分子式 | C₂₀H₂₁N₅O₆·2Na·5/2H₂O |
| 分子量 | 518.43 |
| 规格 | 1ml |
| 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 | Store at -20℃，6 months |
| 运输条件 | 冷冻运输 |
| EC | 814-356-7 |
| SMILES | C1=CC(=CC=C1CCC2=CNC3=C2C(=O)NC(=N3)N)C(=O)N[C@@H](CCC(=O)[O-])C(=O)[O-].C1=CC(=CC=C1CCC2=CNC3=C2C(=O)NC(=N3)N)C(=O)N[C@@H](CCC(=O)[O-])C(=O)[O-].O.O.O.O.O.[Na+].[Na+].[Na+].[Na+] |
| InChIKey | ZCTCZKWJFTYNMZ-WKUCUCPSSA-J |
| InChI | InChI=1S/2C20H21N5O6.4Na.5H2O/c2*21-20-24-16-15(18(29)25-20)12(9-22-16)6-3-10-1-4-11(5-2-10)17(28)23-13(19(30)31)7-8-14(26)27;;;;;;;;;/h2*1-2，4-5，9，13H，3，6-8H2，(H，23，28)(H，26，27)(H，30，31)(H4，21，22，24，25，29);;;;;5*1H2/q;;4*+1;;;;;/p-4/t2*13-;;;;;;;;;/m00........./s1 |
| PubChem CID | 135564527 |
| 靶点 | Antifolate |
| 通路 | Cell Cycle;DNA Damage/DNA Repair |
| 背景说明 | Pemetrexed Disodium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)。 |
| 生物活性 | Pemetrexed disodium hemipenta hydrate is a novel antifolate， the Ki values of the pentaglutamate of 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 Vivo | We observed a synergistic antitumor effect of Treg blockade combined with pemetrexed resulting in prolonged survival. The combination of Treg blockade and pemetrexed was associated with decreased tumor-infiltrating Tregs， increased IL-2 production， dendritic cell maturation， and increased CD3(+)CD8(+)IFN-gamma(+) tumor-infiltrating T cells when compared with mice treated with pemetrexed alone or Treg blockade alone. The survival benefit was abrogated if anti-CD8 mAb was administered simultaneously. Likewise， the survival benefit resulting from the combined Treg blockade with pemetrexed was not observed when immunodeficient mice were used. Therefore， this study suggests that Treg blockade combined with pemetrexed can suppress mesothelioma growth in established tumor in vivo through an immune-mediated process.[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 | 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]. |
| 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] |
| 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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文献和实验相关实验
商品化试剂和培养基均经过严格的质量控制以保证其无菌，但它们在操作过程中可能被污染。请遵循以下指导原则进行无菌操作，避免污染。请始终使用适当的灭菌方法（如高压灭菌器、除菌过滤器）对实验室中配制的任何试剂、培养基或溶液进行灭菌。 无菌操作 请始终用 70% 乙醇擦拭双手和工作区。 将容器、培养瓶、培养板和培养皿放入细胞培养通风橱之前，先用 70% 乙醇擦拭其外部。 不要直接从试剂瓶或培养瓶中倾倒培养基和试剂。 使用无菌玻璃或一次性塑料移液管和移液器操作液体时，每只移液管只能使用一次，以避免
含有结晶水的固体物质，叫做水合物（曾用名：结晶水合物）。结晶水合物中的水分子是以确定量存在的，如FeCl 3 ·6H 2 O、FeSO 4 ·7H 2 O、Ba（OH） 2 ·8H 2 O和ZnSO 4 ·7H 2 O等。因此，结晶水合物是纯净物。水合物中的水分子有各种结合方式。一种是作为配位体，配位在金属离子上，叫配位结晶水。另一种结合在阴离子上，叫阴离子结晶水。例如，CuSO 4 ·5H 2 O加热到113℃，只失去4分子水，加热到258℃才能脱去最后
培养基经高压灭菌后，用经过灭菌的工具（如接种针和吸管等）在无菌条件下接种含菌材料（如样品、菌苔或菌悬液等）于培养基上，这个过程叫做无菌接种操作。在实验室检验中的各种接种必须是无菌操作。 实验台面不论是什么材料，一律要求光滑、水平。光滑是便于用消毒剂擦洗；水平是倒琼脂培养基时利于培养皿内平板的厚度保持一致。在实验台上方，空气流动应缓慢，杂菌应尽量减少，其周围杂菌也应越少越好。为此，必须清扫室内，关闭实验室的门窗，并用消毒剂进行空气消毒处理，尽可能地减少杂菌的数量
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培美曲塞二钠水合物(10mM in Water，无菌)
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