Pemetrexed disodium | LY231514 disodium | 培美曲塞二钠 | DNA/RNA Synthesis | DHFR

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培美曲塞二钠盐 /Pemetrexed disodium {[allProObj[0].p_purity_real_show]}

货号：A206176 同义名： 培美曲塞二钠 / LY231514 disodium

Pemetrexed disodium (LY231514 disodium) 是一种抗叶酸类药物，其五聚谷氨酸形式能抑制胸苷酸合成酶 (TS)、二氢叶酸还原酶 (DHFR) 和甘氨酰胺核糖核苷酸甲酰转移酶 (GARFT)，Ki 值分别为 1.3、7.2 和 65 nM。

Pemetrexed disodium 化学结构
CAS号：150399-23-8

Pemetrexed disodium 3D分子结构
CAS号：150399-23-8

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Pemetrexed disodium 纯度/质量文件产品仅供科研

货号：A206176 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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DNA 亚型比较
DHFR 亚型比较

产品名称	DNA synthesis ↓ ↑	helicase ↓ ↑	RdRp ↓ ↑	ribonucleotide reductase ↓ ↑	tRNA synthetase ↓ ↑	YB-1 ↓ ↑	其他靶点	纯度
Fexinidazole	✔							98%
Daptomycin	✔							98%
Blasticidin S·HCl	✔							98%
Metronidazole	✔							98%
Daunorubicin HCl	+++ DNA synthesis, Ki: 20 nM							98%
Triglycidyl isocyanurate	✔						p53	98+%
Nedaplatin	✔							99%+
Bendamustine	✔							98+%
Trifluridine	✔							98%
Robinetin	✔							99%+
Carboplatin	✔							99%
Cidofovir	✔							99%
Cisplatin	✔							99%
Cytarabine	++++ DNA synthesis, IC50: 16 nM							98%
Acelarin	++++ DNA synthesis, EC50: 0.2 nM							99%+
Oxaliplatin	✔							98%
YK-4-279		✔						99%+
ML216		+ BLM^full-length, IC50: 2.98 μM BLM^636-1298, IC50: 0.97 μM						99%+
RK-33		✔						98%
Brr2-IN-3		✔						99%+
Phen-DC3 Trifluoromethanesulfonate		✔						98%
Favipiravir			✔					97%
Suramin sodium salt			++ RdRp, IC50: 0.26 μM					99%+
Clofarabine				++ Ribonucleotide reductase, IC50: 65 nM				97%
Didox				✔				98%
(E)-3-AP				✔				97%
Halofuginone					+++ prolyl-tRNA synthetase, Ki: 18.3nM			99%+
BC-LI-0186					+++ Leucyl-tRNA synthetase, Kd: 42.1 nM Leucyl-tRNA synthetase, IC50: 46.11 nM			98%
SU056						+ YB-1, IC50: 1.73 μM		98%
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。

产品名称	DHFR ↓ ↑	纯度
Pralatrexate	✔	99%+
Pemetrexed disodium	++++ DHFR, Ki: 7.2 nM	99.9%
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。

Pemetrexed disodium 生物活性

靶点

DHFR

DHFR, Ki:7.2 nM

描述

Pemetrexed disodium is a potent new antifolate which inhibits many folate-dependent reactions that are essential for cell proliferation. Its primary target is thymidylate synthase but it also inhibits folate-dependent enzymes involved in purine synthesis. In the majority of clinical trials of pemetrexed, the dose-limiting toxic effect is neutropenia; other side-effects are mostly gastrointestinal. As a single agent pemetrexed has shown good activity against non-small-cell lung cancer, squamous-cell carcinoma of head and neck, colon cancer, and breast cancer, and it appears to be particularly active in combination with cisplatin against non-small-cell lung cancer and mesothelioma^[3]. Pemetrexed disodium is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively^[4]. As a single agent, pemetrexed exhibits a moderate toxicity profile at a dose of 500 mg/m(2) by 10-minute infusion once every 21 days with myelosuppression being the dose-limiting toxicity^[5].

Pemetrexed disodium 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
211H		Growth Inhibition Assay		IC50=0.07±0.01 μM	24714722
A459	1/2/4 μM	Function Assay	24/48 h	induces G1 phase arrest in dose- and time dependent manner	25743822
A459	1/2/4 μM	Function Assay	48 h	decreases the levels of p-Akt	25743822
A459	4μM	Apoptosis Assay	48 h	induces apoptosis	25743822

Pemetrexed disodium 参考文献

[1]Curtin NJ, Hughes AN. Pemetrexed disodium, a novel antifolate with multiple targets. Lancet Oncol. 2001 May;2(5):298-306

[2]Shih C, Chen VJ, Gossett LS, Gates SB, MacKellar WC, Habeck LL, Shackelford KA, Mendelsohn LG, Soose DJ, Patel VF, Andis SL, Bewley JR, Rayl EA, Moroson BA, Beardsley GP, Kohler W, Ratnam M, Schultz RM. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Res. 1997 Mar 15;57(6):1116-23

[3]Hanauske AR, Chen V, Paoletti P, Niyikiza C. Pemetrexed disodium: a novel antifolate clinically active against multiple solid tumors. Oncologist. 2001;6(4):363-73

Pemetrexed disodium 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.61mL

2.12mL

1.06mL

21.21mL

4.24mL

2.12mL

Pemetrexed disodium 技术信息

CAS号	150399-23-8
分子式	C₂₀H₁₉N₅Na₂O₆
分子量	471.374

别名	培美曲塞二钠 ;LY231514 disodium
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

H₂O: 100 mg/mL(212.15 mM)，配合低频超声，并水浴加热至45℃助溶

动物实验配方

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

211H		Growth Inhibition Assay		IC50=0.07±0.01 μM	24714722
A459	1/2/4 μM	Function Assay	24/48 h	induces G1 phase arrest in dose- and time dependent manner	25743822
A459	1/2/4 μM	Function Assay	48 h	decreases the levels of p-Akt	25743822
A459	4μM	Apoptosis Assay	48 h	induces apoptosis	25743822
A549	1 μM	Cell Viability Assay	48 h	enhances simvastatin inhibited viability	26334320
A549	1 μM	Function Assay	24 h	enhances autophagy cotreated with simvastatin	26334320
A549	1 μM	Apoptosis Assay	24 h	induces apoptosis cotreated with simvastatin	26334320
A549	1 μM	Function Assay	48 h	increases AMPK phosphorylation and a concomitant decrease in AKT and mTOR phosphorylation cotreated with simvastatin	26334320
A549	0.234 mM	Growth Inhibition Assay	24 h	growth inhibition=10﹪	25975637
A549	0.234 mM	Growth Inhibition Assay	48 h	growth inhibition=30﹪	25975637
A549	0.234 mM	Growth Inhibition Assay	72 h	growth inhibition=50﹪	25975637
A549	1-1000 nM	Cell Viability Assay	72 h	IC50=137 nM	25145669
A549	1 μM	Cell Viability Assay	48 h	produces a synergistic inhibitory effect on the cell growth combined with simvastatin	25096993
A549	1 μM	Apoptosis Assay	48 h	enhances caspase-dependent apoptosis combined with simvastatin	25096993
A549	1 μM	Function Assay	48 h	enhances intracellular ROS production combined with simvastatin	25096993
A549	1 μM	Function Assay	48 h	leads to mitochondrial dysfunction combined with simvastatin	25096993
A549	2.5/5/10 μM	Function Assay	48 h	increases Noxa expression significantly	24991768
A549	2.5 μM	Function Assay	48 h	induces caspase-9, caspase-3 and poly (ADP-ribose) polymerase (PARP) cleavage	24991768
A549	2.5/5/10 μM	Function Assay	48 h	downregulates Mcl-1	24991768
A549	2.5 μM	Apoptosis Assay	48 h	induces apoptosis	24991768
A549	5 μM	Function Assay	8 h	increases Mcl-1 ubiquitination levels	24991768
A549	1 µM	Function Assay	4/8/12/24/48 h	increases the level of phosphorylated Akt in a time dependent manner	24847863
A549	0.1/0.3/1 μM	Function Assay	48 h	increases the level of phosphorylated Akt in a dose dependent manner	24847863
A549	0.1/0.3/1 μM	Apoptosis Assay	48 h	induces apoptosis in a dose dependent manner	24847863
A549	0.1/0.3/1 μM	Function Assay	48 h	increases the ratio of S-phase population	24847863
A549	0.1/0.3/0.5/1 μM	Cell Viability Assay	24/48 h	inhibits cell viability dose and time dependently	24626722
A549	0.1/0.3/0.5/1 μM	Function Assay	24/48 h	produces the formation of AVOs in a dose-dependent manner	24626722
A549		Growth Inhibition Assay	96 h	IC50=1.35 μM	24348854
A549/PEM-1.6		Growth Inhibition Assay	96 h	IC50=5.03 μM	24348854
A549/PEM-16		Growth Inhibition Assay	96 h	IC50=51.45 μM	24348854
A549/PEM-6.4		Growth Inhibition Assay	96 h	IC50=23.39 μM	24348854
BXPC-3		Growth Inhibition Assay		IC50=39.86±1.68 μM	22977607
BXPC-3	39.86 μM	Function Assay	24 h	induces S arrest (P<0.05) and decreases the number of cells in the G2/M phase	22977607
BXPC-3	39.86 μM	Function Assay	24 h	enhances EGFR phosphorylated levels, and the protein levels	22977607
BXPC-3	39.86 μM	Function Assay	24 h	enhances EGFR, HER3 and AKT phosphorylation levels	22977607
DM-3		Growth Inhibition Assay	48 h	proportion of live cells=101.3±2.8 %	23840376
H1299	1-1000 nM	Cell Viability Assay	72 h	IC50=178 nM	25145669
H1299		Growth Inhibition Assay		IC50=1.84 μM	24418519
H1792	2.5/5/10 μM	Function Assay	48 h	increases Noxa expression significantly	24991768
H1792	2.5 μM	Function Assay	48 h	induces caspase-9, caspase-3 and poly (ADP-ribose) polymerase (PARP) cleavage	24991768
H1792	2.5/5/10 μM	Function Assay	48 h	downregulates Mcl-1	24991768
H1993		Growth Inhibition Assay		IC50=0.17 μM	24418519
H2052		Growth Inhibition Assay		IC50=0.57±0.34 μM	24714722
H226	1-10 μg/ml	Cell Viability Assay	72 h	IC50>10 μg/ml	24378576
H2452		Growth Inhibition Assay		IC50＞100 μM	24714722
H28		Growth Inhibition Assay		IC50=0.07±0.02 μM	24714722
H290	1-10 μg/ml	Cell Viability Assay	72 h	IC50>10 μg/ml	24378576
HCT116		Growth Inhibition Assay	72 h	IC50=0.049 ± 0.013 μM	23959460
HeLa	0.234 mM	Growth Inhibition Assay	24 h	growth inhibition=5﹪	25975637
HeLa	0.234 mM	Growth Inhibition Assay	48 h	growth inhibition=10﹪	25975637
HeLa	0.234 mM	Growth Inhibition Assay	72 h	growth inhibition=20﹪	25975637
HepG2	0.1–100 μM	Cell Viability Assay	72 h	high concentrations of pemetrexed at (10/100 μM) only slightly inhibits HepG2 cell survival	25446102
HepG2	0.1–100 μM	Apoptosis Assay	72 h	induces apoptosis slightly at high concerntration	25446102
HepG3	0.1–100 μM	Function Assay	48 h	induces p62 downregulation as well as Beclin-1 and LC3B-II upregulation	25446102
HepG3	0.1–100 μM	Function Assay	48 h	activates cyto-protective autophagy	25446102
HepG3	10 μM	Function Assay	48 h	upregulates phosphorylated (p-) MEK1/2 (Ser217/221) and p-ERK1/2 (Thr202/Tyr204)	25446102
HT-29		Growth Inhibition Assay	72 h	IC50=10.07 ± 0.94 μM	23959460
HT-29	0.05 μM	Function Assay	72 h	increases the percentage of cells in the S phase	23959460
JL-1		Growth Inhibition Assay	48 h	proportion of live cells=98.2±2.2 %	23840376
Jurkat		Growth Inhibition Assay	48 h	proportion of live cells=76.7±4.3 %	23840376
LoVo		Growth Inhibition Assay	72 h	IC50=0.032 ± 0.002 μM	23959460
LoVo	0.05 μM	Function Assay	72 h	increases the percentage of cells in the S phase	23959460
M-14-K		Growth Inhibition Assay	48 h	proportion of live cells=81.8±12.9 %	23840376
MES01		Growth Inhibition Assay		IC50＞100 μM	24714722
MES04		Growth Inhibition Assay		IC50＞100 μM	24714722
MG-63	0.01-100 μM	Cell Viability Assay	72 h	inhibits cell viability dosedependently	25152399
MSTO-211	1 μM	Cell Viability Assay	48 h	produces a synergistic inhibitory effect on the cell growth combined with simvastatin	25096993
MSTO-211	1 μM	Apoptosis Assay	48 h	enhances caspase-dependent apoptosis combined with simvastatin	25096993
MSTO-211	1 μM	Function Assay	48 h	enhances intracellular ROS production combined with simvastatin	25096993
MSTO-211	1 μM	Function Assay	48 h	leads to mitochondrial dysfunction combined with simvastatin	25096993
MSTO-211H	1 μM	Cell Viability Assay	48 h	enhances simvastatin inhibited viability	26334320
MSTO-211H	1 μM	Function Assay	24 h	enhances autophagy cotreated with simvastatin	26334320
MSTO-211H	1 μM	Apoptosis Assay	24 h	induces apoptosis cotreated with simvastatin	26334320
MSTO-211H	1 μM	Function Assay	48 h	increases AMPK phosphorylation and a concomitant decrease in AKT and mTOR phosphorylation cotreated with simvastatin	26334320
MSTO-211H	1-10 μg/ml	Cell Viability Assay	72 h	IC50~0.04 μg/ml	24378576
PANC-1		Growth Inhibition Assay		IC50=83.76±0.19 μM	22977607
PANC-1	84 μM	Function Assay	24 h	enhances EGFR phosphorylated levels, and the protein levels	22977607
PANC-1	84 μM	Function Assay	24 h	enhances EGFR, HER3 and AKT phosphorylation levels	22977607
PC9		Growth Inhibition Assay	72 h	IC50=16.05±1.85 nM	24840891
PC9	16 nM	Function Assay	72 h	induces S-phase arrest	24840891
PC9	16 nM	Apoptosis Assay	72 h	induces 14.54﹪ apoptosis	24840891
PC9/GR		Growth Inhibition Assay	72 h	IC50=4.94±0.440 μM	24840891
PC9/GR	4.94 μM	Function Assay	72 h	induces S-phase arrest	24840891
PC9/GR	4.94 μM	Apoptosis Assay	72 h	induces 19.54﹪ apoptosis	24840891
PC9/GR	4.94 μM	Function Assay	72 h	increases p-ERK levels	24840891
PC9/GR	4.94 μM	Function Assay	72 h	increases p-AKT levels	24840891
STAV-AB		Growth Inhibition Assay	48 h	proportion of live cells=64.4±21.8 %	23840376
STAV-FCS		Growth Inhibition Assay	48 h	proportion of live cells=88.1±8.9 %	23840376
SW1116		Growth Inhibition Assay	72 h	IC50=1.70 ± 0.03 μM	23959460
SW620		Growth Inhibition Assay	72 h	IC50=1.09 ± 0.01 μM	23959460
T47D	0.234 mM	Growth Inhibition Assay	24 h	growth inhibition=10﹪	25975637
T47D	0.234 mM	Growth Inhibition Assay	48 h	growth inhibition=20﹪	25975637
T47D	0.234 mM	Growth Inhibition Assay	72 h	growth inhibition=30﹪	25975637
U20S	0.01-100 μM	Cell Viability Assay	72 h	inhibits cell viability dosedependently	25152399
Vero	0.234 mM	Growth Inhibition Assay	24 h	growth inhibition=5﹪	25975637
Vero	0.234 mM	Growth Inhibition Assay	48 h	growth inhibition=10﹪	25975637
Vero	0.234 mM	Growth Inhibition Assay	72 h	growth inhibition=20﹪	25975637
WiDr		Growth Inhibition Assay	72 h	IC50=0.019 ± 0.002 μM	23959460
Y-meso14	1-10 μg/ml	Cell Viability Assay	72 h	IC50>10 μg/ml	24378576
ZL-34		Growth Inhibition Assay	48 h	proportion of live cells=95.7±6.5 %	23840376

培美曲塞二钠盐 /Pemetrexed disodium {[allProObj[0].p_purity_real_show]}

Pemetrexed disodium 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Pemetrexed disodium 质控信息

Pemetrexed disodium 生物活性

Pemetrexed disodium 细胞研究

Pemetrexed disodium 参考文献

Pemetrexed disodium 实验方案

Pemetrexed disodium 技术信息

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培美曲塞二钠盐 /Pemetrexed disodium {[allProObj[0].p_purity_real_show]}

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最近浏览的产品

大规格询价

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总药量计算器

工作液计算器

细胞研究

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