Catalog No.S1135 Synonyms: LY-231514
Molecular Weight(MW): 471.37
Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively.
Cited by 6 Publications
3 Customer Reviews
Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
Cancer Res 2014 74(21), 5948-54. Pemetrexed purchased from Selleck.
Purity & Quality Control
Choose Selective DHFR Inhibitors
|Description||Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively.|
Pemetrexed disodium shows the antiproliferative activity in CCRF-CEM leukemia, GC3/C1 colon carcinoma, and HCT-8 ileocecal carcinoma cells with IC50 of 25 nM, 34 nM and 220 nM, respectively.  A recent study shows that cisplatin plus Pemetrexed combined with SOCS-1 gene delivery shows the antitumor effect by inhibition of cell proliferation, invasiveness, and induction of apoptosis in MPM cells infected with adenovirus-expressing SOCS-1 vector. 
|In vivo||In the human H460 non-small cell lung carcinoma xenograft, Pemetrexed disodium produces a duration-dependent tumor growth delay (TGD). |
Enzyme Assays and Methods. :TS activity is assayed using a spectrophotometric method, which involved monitoring the increase in absorbance at 340 nm resulting from formation of the product, 7,8-dihydrofolate. The assay buffer contains 50 mM N-tris[hydroxymethyljmethyl-2-aminoethanesulfonic acid, 25 mM MgC12, 6.5 mM formaldehyde, 1 mM EDTA, and 75 mM 2-mercaptoethanol, pH 7.4. The concentrations of deoxyuridylate monophosphate, 6R-MTHF, and hIS are 100 μM, 30μM and 30 nM (1.7 milliunits/mL), respectively. At the 6R-MTHF concentration, an uninhibited reaction and six concentrations of inhibitor are assayed. Ki app values are determined by fitting the data to the Morrison equation using nonlinear regression analysis with the aid of the program ENZFITTER. Ki values are calculated using the equation: Ki app= Ki(1 + [S]/Km), where [S] is equal to 30 μM and Km is equal to 3 μM. DHFR activity is assayed spectrophotometrically by monitoring the dis appearance of the substrates NADPH and 7,8-dihydrofolate at 340 nm. The reaction takes place at 25°C in 0.5 mL of 50 mM potassium phosphate buffer, which contains 150 mM KC1 and 10 nM 2-mercaptoethanol, pH 7.5, and 14 nM (0.34 milliunitlmL) DHFR. The NADPH concentration is 10 μM and 7,8-dihydrofolate is varied at 5, 10, or 15 μM. At each 7,8-dihydrofolate concentration, an uninhibited reaction and seven concentrations of inhibitor are assayed. The ENZFITI'ER microcomputer program is used to obtain Ki app values by fitting the data to the Morrison equation by nonlinear regression analysis. Ki app= Ki(1 + [S]/Km), where [S] is equal to the concentration of 7,8-dihydrofolate used and Km of 7,8-dihydrofolate is equal to 0.15 μM. GARFT activity is assayed spectrophotometrically by monitoring the increase of absorbance resulting from formation of the product 5,8-dideazafolate at 295 nm. The reaction solvent contains 75 mM HEPES, 20% glycerol, and 50 mM a-thioglygerol, pH 7.5, at 25°C. The concentrations of substrates and enzyme used are 10 μM α,β-glycinamide ribonucleotide, 0-10 μM 10-formyl-5,8-dideazafolic acid, and 10 nM (1.9 milliunits/mL) GARFT. Ki values are calculated using the Enzyme Mechanism program of the Beckman DU640 spectrophotometer, which uses nonlinear regression analysis to fit data to the Michaelis-Menten equation for competitive inhibition.
|In vitro||Water||94 mg/mL (199.41 mM)|
|In vivo||Add solvents to the product individually and in order:
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02357147||Active, not recruiting||Mesothelioma, Malignant||Morphotek||November 4, 2015||Phase 2|
|NCT02185690||Not yet recruiting||Lungcancer||University Health Network, Toronto|Novartis Pharmaceuticals||March 2017||Phase 1|
|NCT02964689||Not yet recruiting||Advanced Non-small Cell Lung Cancer|KRAS Gene Mutation|Lung Cancer||Swiss Group for Clinical Cancer Research||March 2017||Phase 1|
|NCT02998528||Recruiting||Non Small Cell Lung Cancer||Bristol-Myers Squibb||January 2017||Phase 3|
|NCT03023319||Recruiting||Carcinoma, Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer||Nagla Karim|University of Cincinnati||January 2017||Phase 1|
|NCT03003962||Not yet recruiting||Non Small Cell Lung Carcinoma (NSCLC)||AstraZeneca||January 2017||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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