货号:A209789
同义名:
LY231514 disodium heptahydrate; Pemetrexed(sodium salt hydrate)
Pemetrexed disodium heptahydrate是一种新型抗叶酸剂,其五聚谷氨酸形式对胸苷酸合成酶(TS)的Ki值为1.3 nM,对二氢叶酸还原酶(DHFR)为7.2 nM,对甘氨酰胺核糖核苷酸甲酰基转移酶(GARFT)为65 nM。


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| 产品名称 | DHFR ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Pralatrexate | ✔ | 99%+ | |||||||||||||||||
| Pemetrexed disodium |
++++
DHFR, Ki: 7.2 nM |
99% | |||||||||||||||||
| Pyrimethamine |
++
DHFR, IC50: 15.4 nM |
98% HPLC | |||||||||||||||||
| Pemetrexed |
++++
DHFR , Ki: 7.2 nM |
99+% | |||||||||||||||||
| Methotrexate |
+
hDHFR, IC50: 24 nM |
99% (contain ~10%water) | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Pemetrexed disodium is a guanine-derived antineoplastic agent that functions as a nucleic acid synthesis inhibitor through its binding to, and inhibition of, thymidylate synthase. |
| Concentration | Treated Time | Description | References | |
| CL141 lung cancer cells | 100 nM | 24 hours | To determine the effect of pemetrexed on PD-L1 expression and T cell activation | J Immunother Cancer. 2020 Nov;8(2):e001392. |
| A549 cells | 250 nM | 48 hours | Enhanced PD-L1 and HLA-G expression and glycosylation, and increased CTL cytotoxicity against A549 cells | Cancer Sci. 2023 Jul;114(7):2761-2773. |
| H1975 cells | 50 nM | 48 hours | Enhanced PD-L1 and HLA-G expression and glycosylation, and increased CTL cytotoxicity against H1975 cells | Cancer Sci. 2023 Jul;114(7):2761-2773. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Syngeneic mouse models | Intraperitoneal injection | 50 mg/kg | Every 4 days for two cycles | To evaluate the combination effect of pemetrexed and anti-PD-L1 antibody on tumor growth inhibition | J Immunother Cancer. 2020 Nov;8(2):e001392. |
| NOD.Cg-PrkdcSCID/ll2rgtm1vst/Vst (NPG) mice | A549-Luc xenograft model | Tail vein injection | 50 mg/kg | Once weekly for 2 weeks | Pemetrexed combined with dual immune checkpoint blockade (anti-PD-L1 and anti-HLA-G) significantly promoted CTL-mediated cytotoxicity and inhibited tumor growth | Cancer Sci. 2023 Jul;114(7):2761-2773. |
[2]Rollins KD, Lindley C. Pemetrexed: a multitargeted antifolate. Clin Ther. 2005 Sep;27(9):1343-82.
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.67mL 0.33mL 0.17mL |
8.37mL 1.67mL 0.84mL |
16.74mL 3.35mL 1.67mL |
|
| CAS号 | 357166-29-1 |
| 分子式 | C20H33N5Na2O13 |
| 分子量 | 597.48 |
| SMILES Code | O=C([O])CC[C@@H](C([O-])=O)NC(C1=CC=C(CCC2=CNC(N=C(N)N3)=C2C3=O)C=C1)=O.[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[Na+].[Na] |
| MDL No. | MFCD09029394 |
| 别名 | LY231514 disodium heptahydrate; Pemetrexed(sodium salt hydrate) |
| 运输 | 蓝冰 |
| InChI Key | QJVSMHJWAOSBMD-MYXYZBIASA-L |
| Pubchem ID | 135564751 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
H2O: 100 mg/mL(167.37 mM),配合低频超声助溶 |
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