Product Data Sheet Pemetrexed disodium hemipenta hydrate(1:2:2.5)Product Name:CAS No.: Cat.No.:Cat. No.:MWt:Formula:Purity :357166-30-4HY-13781HY13781516.41C20H19N5Na2O6>98%Solubility:DMSOMechanisms: Pathways:Cell Cycle/DNA Damage; Target:Antifolate Biological Activity:Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2PdilifldiblifTSDHFRdGARFTihKif13M72nM and 65 nM, respectively. IC50 Value: 1.3 nM(Ki for TS); 7.2nM(DHFR); 65 nM(GARFT) Target: Antifolate in vitro: The Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibitionagainst TS, DHFR, and GARFT, respectively. In contrast, although a similar high level of inhibitorypotency was observed for the parent monoglutamate against DHFR (7.0 nM), the inhibitionconstants (Ki) for the parent monoglutamate are significantly weaker for TS (109 nM) andGARFT(9300nM)TheparentmonoglutamateLY231514inhibitedrhTSwithaKiof109nMwhenGARFT(9,300 nM).The parent monoglutamate LY231514 inhibited rhTS with a Ki of 109 nM whenthe monoglutamated form of the substrate (6R-MTHF) (6[R]-5,l0-meth ylenetetrahydrofolate) wasused. This is in good agreement with the Ki value generated earlier for rmTS (Ki= 340 nM)[1]. in vivo: pemetrexed effec...References:[1]. Shih C, Chen VJ, Gossett LS, LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibitsmultiple folate-requiring enzymes. Cancer Res. 1997 Mar 15;57(6):1116-23. [2]. Müller C, Reddy JA, Leamon CP, Effects of the antifolates pemetrexed and CB3717 on thetissue distribution of (99m)Tc-EC20 in xenografted and syngeneic tumor-bearing mice. Mol Pharm.2010 Apr 5;7(2):597-604. [3]. Rudin CM, Brahmer JR, Juergens RA, Phase 2 study of pemetrexed and itraconazole assecond-line therapy for metastatic nonsquamous non-small-cell lung cancer.J Thorac Oncol. 2013May;8(5):619-23. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 08540,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr