| Size | Price | Stock | Qty |
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| 50mg |
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| 500mg |
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Purity: ≥98%
Pemetrexed Disodium Hydrate (LY-231514; HSDB-7316; trade name Alimta), the hydrated disodium salt of Pemetrexed which is a synthetic pyrimidine-based antifolate, is a novel antifolate and antimetabolite anticancer drug targeting TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. Pemetrexed exhibits high autitumor activity in a broad range of tumors such as NSCLC/non-small cell lung carcinoma, malignant mesothelioma, and carcinomas of the breast, colorectum, uterine cervix, head and neck, and bladder.
| ln Vitro |
Pemetrexed (LY231514) disodium neoplasm is a novel family of classical antifolate medications whose anti-activity may result from its polyglutamate promoter's simultaneous and cooperative suppression of multiple essential folate enzyme needs. One of the most well-known enzyme FPGS substrates is pemetrexed (LY231514), with a Km of 1.6 μM and a Vmax/Km of 621. The selectivity and antitumor efficaciousness of LY231514 may be determined by its polyglutamate and polyglutamic acid auxiliaries. Although TS is inhibited by LY23l5l4 alone (Ki=340 nM in recombinant mice), LY23l5l4's glutamic acidity is strong. One of the most potent folic acid TS is LY231514, which is 100 times higher (Ki=3.4 nM) [1].
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| ln Vivo |
Statistically speaking, the mice in the PC61 plus pemetrexed group survived longer than the other groups. According to survival analysis, mice treated with PC61 with pemetrexed had a considerably higher survival rate than mice treated with PC61 alone, rat IgG plus pemetrexed, or no therapy at all [2].
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Most sources consider breastfeeding to be contraindicated during maternal high-dose antineoplastic drug therapy. The manufacturer recommends that mothers should not to breastfeed during treatment with pemetrexed and for one week after the last dose. Chemotherapy may adversely affect the normal microbiome and chemical makeup of breastmilk.[1] Women who receive chemotherapy during pregnancy are more likely to have difficulty nursing their infant.[2] ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. 28170295 |
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| References |
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| Additional Infomation |
Pemetrexed(2-) is a dicarboxylic acid dianion obtained by deprotonation of both carboxy groups of pemetrexed. It is a dicarboxylic acid dianion and a N-acyl-L-alpha-amino acid anion. It is a conjugate base of a pemetrexed.
A guanine-derived ANTINEOPLASTIC AGENT that functions as a NUCLEIC ACID SYNTHESIS INHIBITOR through its binding to, and inhibition of, THYMIDYLATE SYNTHASE. Drug Indication Malignant pleural mesotheliomaAlimta in combination with cisplatin is indicated for the treatment of chemotherapy-naïve patients with unresectable malignant pleural mesothelioma. Non-small-cell lung cancer Alimta in combination with cisplatin is indicated for the first-line treatment of patients with locally advanced or metastatic non-small-cell lung cancer other than predominantly squamous cell histology. Alimta is indicated as monotherapy for the maintenance treatment of locally advanced or metastatic non-small-cell lung cancer other than predominantly squamous cell histology in patients whose disease has not progressed immediately following platinum-based chemotherapy. Alimta is indicated as monotherapy for the second line treatment of patients with locally advanced or metastatic non-small-cell lung cancer other than predominantly squamous cell histology. |
| Molecular Formula |
C20H21N5O6.5/2H2O.2NA
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| Molecular Weight |
516.42
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| Exact Mass |
425.133
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| CAS # |
357166-30-4
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| Related CAS # |
Pemetrexed;137281-23-3;Pemetrexed disodium;150399-23-8
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| PubChem CID |
135916113
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| Appearance |
White to off-white solid powder
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| LogP |
1.5
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
737
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC(=CC=C1CCC2=CNC3=C2C(=O)NC(=N3)N)C(=O)N[C@@H](CCC(=O)[O-])C(=O)[O-]
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| InChi Key |
QJVSMHJWAOSBMD-MYXYZBIASA-L
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| InChi Code |
InChI=1S/C20H21N5O6.2Na.7H2O/c21-20-24-16-15(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;;;;;;;;;/h1-2,4-5,9,13H,3,6-8H2,(H,23,28)(H,26,27)(H,30,31)(H4,21,22,24,25,29);;;7*1H2/q;2*+1;;;;;;;/p-2/t13-;;;;;;;;;/m0........./s1
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| Chemical Name |
sodium (S)-2-(4-(2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido)pentanedioate heptahydrate.
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| Synonyms |
LY-231514 Disodium Hydrate; LY231514; LY 231514; Pemetrexed, US brand name: ALIMTA
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 33.33 mg/mL (64.54 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9364 mL | 9.6820 mL | 19.3641 mL | |
| 5 mM | 0.3873 mL | 1.9364 mL | 3.8728 mL | |
| 10 mM | 0.1936 mL | 0.9682 mL | 1.9364 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01473563 | Completed Has Results | Drug: Pemetrexed | Nonsquamous Non-Small Cell Neoplasm of Lung |
Eli Lilly and Company | December 2011 | Phase 2 |
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