Autres

Applications Α labelled metabolite of Tamoxifen (T006000).
References Sun, D., et al.: Breast Cancer Res., 8(4), (2006), Zheng, Y., et al.: Drug Metab. Dispos., 35, 1942 (2007),

Applications Palbociclib N-Aldehyde is an intermediate in synthesizing Palbociclib N-β-D-Glucuronide Sodium Salt (P139910), a derivative of Palbociclib (P139900) which is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.
References Finn, R., et al.: Breast Cancer Res., 11, 5 (2009)

Impurity Atenolol EP Impurity H
Applications 2-[4-[(2RS)-2-Hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]acetonitrile is an impurity of Atenolol (A790075), a cardioselective β-adrenergic blocker. Atenolol EP Impurity H
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984);

Applications (S)-2-((S)-4-Methyl-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamido)-3-phenylpropanoic Acid is an intermediate for Carfilzomib (C183460), which is a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma.
References Fostier, K., et al.: Oncotargets. Therap., 5, 237 (2012); Geurink, P.P., et al.: J. Med. Chem., 56, 1262 (2013); McCormack, P.L., et al.: Drugs., 72, 2023 (2012);

Applications (2E)-2-Cyano-3-(3-ethoxy-4-hydroxy-5-nitrophenyl)-N,N-diethyl-2-propenamide is an impurity of Entacapone (E558500), a peripherally acting inhibitor of catechol-O-methyl transferase (COMT), an enzyme involved in the metabolism of catecholamine neurotransmitters and related drugs. Antiparkinsonian.
References Karlsson, M., et al.: J. Pharm. Biomed. Anal., 10, 593 (1992), Nissinen, E., et al.: Arch. Pharmacol., 346, 262 (1992), Wikberg, T., et al.: Eur. J. Drug Metab. Pharmacokinet., 18, 359 (1993),

Applications An impurity of Nintedanib, which is an antifibrotic drug.
References Holdsworth, G.; et al.: Scientific Reports, 7, 1 (2017)

Applications Zafirlukast m-Tolyl Isomer is a positional isomer and impurity of the cysteinyl leukotriene type 1 receptor antagonist, Zafirlukast (D226955).
References Krishnaiah, C. et al.: Anal. Chem. Ind. J., 8, 471 (2009); Madhavi, A. et al.: Chromatographia, 70, 233 (2009); Goverdhan, G. et al.: J. Pharmac. Biomed. Anal., 49, 895 (2009);

Applications (αE)-α-[(3,4-Dihydroxy-5-nitrophenyl)methylene]-β-oxo-1-piperidinepropanenitrile is an impurity of Entacapone (E558500), a peripherally acting inhibitor of catechol-O-methyl transferase (COMT), an enzyme involved in the metabolism of catecholamine neurotransmitters and related drugs. Antiparkinsonian.
References Karlsson, M., et al.: J. Pharm. Biomed. Anal., 10, 593 (1992), Nissinen, E., et al.: Arch. Pharmacol., 346, 262 (1992), Wikberg, T., et al.: Eur. J. Drug Metab. Pharmacokinet., 18, 359 (1993),

Applications Methyl 4-Hydroxyphenylacetate has been shown to have potent inhibitory activity against tobacco mosaic virus (TMV).
References Shen, S., Li, W., Wang, J.: Nat. Prod. Res., 27, 2286 (2013); Golovleva, L.A., et. al.:

Applications N-[4-[[(Z)-(1,2-Dihydro-2-oxo-3H-indol-3-ylidene)phenylmethyl]amino]phenyl]-N,4-dimethyl-1-piperazineacetamide was used in the study to discover a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth. N-[4-[[(Z)-(1,2-Dihydro-2-oxo-3H-indol-3-ylidene)phenylmethyl]amino]phenyl]-N,4-dimethyl-1-piperazineacetamide is an impurity of Intedanib (I666650), which is an antitumor agent.
References Edupuganti, R., et al.: Bioorg. Med. Chem., 25, 2609 (2017); Sun, L., et al.: J. Med. Chem., 41, 2588 (1998); Xie, H., et al.: J. Med. Chem., 50, 4898 (2007); Hilberg, F., et al.: Cancer Res., 68, 4774 (2008); Roth, G., et al.: J. Med. Chem., 58, 1053 (2015)

Applications: Labelled Almotriptan (A575200). Almotriptan is a serotonin 5HT1B /1D-receptor agonist used for treatment of migraine.
References Fleishaker, J.C., et al.: Clin. Pharmacol. Ther., 67, 498 (2000), Kamali, F., et al.: Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs, 2, 197 (2000), Dodick, D.W., et al.: Expert Opin.Pharmacother., 4, 1157 (2003)