Pemetrexed is a high affinity dihydrofolate reductase inhibitor (Ki = 7 nM). Pemetrexed also inhibits thymidylate synthase, AICART and glycinamide ribonucleotide formyltransferase (Ki values are 109 nM, and 3.5 μM and 9.3 μM, respectively). Indirectly activates AMPK. Pemetrexed inhibits proliferation of cancer cell lines in vitro.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 45 mg/mL|
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
Yan, et al. J Med Chem. 2014;57: 2611. PMID: 24564570.
|Related Antifolate Products|
|Pemetrexed Disodium Hydrate
Pemetrexed Disodium Hydrate is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.
Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.
Trimethoprim is a bacteriostatic antibiotic mainly used in the prophylaxis and treatment of urinary tract infections.
|Folinic acid calcium salt
Folinic acid is an adjuvant used in cancer chemotherapy involving the compound methotrexate.
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