Autres

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 The trans-isomer used in the improved process for the production and purification of Bimatoprost (B386800).

Applications An alkyladamantane derivative that are biotransformed via strains of Pseudomonas. It is used to study alkyladamantane adsorption on graphitized thermal carbon black.
References Yashkin, S.N. et al.: Rus. Che,. Bull., 57, 2472 (2008); Slepen’kin, A. et al.: Nefeckhim., 33, 406 (1993);

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 Labelled analogue of cis-Entacapone, the (Z)-Isomer of Entacapone (E558500) polymorphic form B. 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 (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),

Impurity Fulvestrant Impurity E;
Applications Fulvestrant (F862500) impurity E.

Applications (Z)-4-Hydroxy Tamoxifen O-β-D-Glucuronide is an active metabolite of Tamoxifen (T006000).
References Ogura, K. et al.: Biochem. Pharmacol., 71, 1358 (2006); Nishiyama, T. et al.: Biochem. Pharmacol., 63, 1817 (2002); McCague, R. et al.: Biochem. Pharmacol., 39, 1459 (1990);

Impurity Leuprolide Acetate EP Impurity B TFA salt
Applications Synthetic nonapeptide agonist analog of LH-RH. Antineoplastic (hormonal).
References Vilchez-Martinez, J.A., et al.: Biochem. Biophys. Res. Commun., 59, 1226 (1974), Sennello, L.T., et al.: J. Pharm. Sci., et al.: 75, 158 (1986), Wheeler, J.M., et al.: Am.J. Obstet. Gynecol., 167, 1367 (1992), Eri, L.M., et al.: J. Urol., 150, 359 (1993),

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)