Toxicology

Applications Dydrogesterone (D826000) intermediate. Used in the preparation of 10α-steroids.

Applications Clindamycin (C580000) derivative. Used in the preparation of Clindamycin impurities.

Applications An intermediate in the synthesis of Epothilones. Epothilones are polyketide natural products that inhibit cancer cells by a mechanism similar to paclitaxel, and also are effective against paclitaxel-resistant tumours. Epothilone D is in phase I clinical testing of in patients with advanced solid tumours. Epothilone D is a cytotoxic macrolide that stabilises malignant cells' microtubules and arrests mitosis, a characteristic it shares with other epothilones. They bind to the same hepatic sites as does paclitaxel (Taxol) in a 1:1 stoichiometric ratio of a, b-tubulin heterodimers.
References Hoee, G., et al.: Pure Appl. Chem., 71, 11, 2019 (1999), Giannakakou, P., et al.: Proc. Natl. Acad. Sci. USA, 97, 2904 (2000)

Applications Labelled Bexarotene (B336750). Used as an antineoplastic. A selective retinoid X receptor (RXR) agonist.
References Boehm, M.F., et al.: J. Med. Che., 37,2930 (1994), Gottardis, M.M., et al.: Cancer Res., 56, 5566 (1996), Mukherjee, R., et al.: Nature, 386, 407 (1997), Miller, V.A., et al.: J. Clin. Oncol., 15, 790 (1997)

Applications MRX-2843, is an orally available small-molecule inhibitor of both MERTK and FLT3.
References Minson, K. A. et al.: JCI Insight. 2016 Mar;1(3):e85630.;

Applications Methyl 1,4-Dihydro-4-(2’-trifluoromethyl)phenyl-pyridine-3-carboxylate-5-ethyl Carboxamide (cas# 887407-06-9) is a compound useful in organic synthesis.

Applications (3R,5S)-5-(6-Cyclopropyl-10-fluoro-7,8-dihydrobenzo[k]phenanthridin-8-yl)-3,5-dihydroxypentanoic Acid Sodium Salt is an impurity of Pitavastatin (P531000), a competitive inhibitor of HMG-CoA reductase. Antilipemic.
References Aoki, T., et al.: Arzneim.-Forsch., 47, 904 (1997); Yamada, I., et al.: Xenobiotica, 33, 789 (2003); Park, S., et al.: Clin. Ther., 27, 1074 (2005)

Applications 6-Chloropurine 2'-Deoxy-Beta-D-ribofuranoside Diacetate is an intermediate in the synthesis of anti-hepatitis C virus agents.
References Patil, V.M., et. al.: Lett. Drug Des. Discov., 7, 139 (2010)

Stability Hygroscopic, Moisture Sensitive
Applications 1-​[1-​(4-​Chlorobenzoyl)​-​5-​hydroxy-​2-​methyl-​1H-​indole-​3-​acetate]β-​D-​Glucopyranuronic Acid is an analog of Indomethacin Acyl-β-D-glucuronide a metabolite of Indomethacin (I641000). Acyl glucuronides have been implicated in the toxicity of many xenobiotics and marketed drugs.
References Abid, A., et al.: Biochem. Pharmacol., 50, 557 (1995), Gamage, N., et al.: Toxicol. Sci., 90, 5 (2006), Cerveny, L., et al.: Drug Metab. Dispos., 35, 1032 (2007), Hayeshi, R., et al.: Eur. J. Pharm. Sci., 35, 383 (2008),

Applications Labelled Azathioprine (A803350). An immunosuppressive antimetabolite. Also active as disease modifying antirheumatic drug (DMARD).
References Mitrou, P.S., et al.: Arzneim.-Forsch., 29, 483, 662 (1979), Ding, T.L., et al.: Drug. Metab. Dispos., 7, 373 (1979), Chan, G.L.C., et al.: Pharmacotherapy, 7, 165 (1987), Sandborn, W.J., et al.: : Scand. J. Gastroenterol., 33, Suppl. 225, 92 (1998,)

Applications O-Desacetyl O-Propionyl Famciclovir is an impurity of Famciclovir (F101125); a compound that is used as an antiviral and is a prodrug of Penciclovir (P221500).
References Hodge, V.R.A., et al.: Antimicrob. Ag. Chemother., 33, 1765 (1989)

Applications dl-threo-Ritalinic Acid Isopropyl Ester Hydrochloride is an analog of Methylphenidate (M325880), a controlled substance (stimulant). CNS stimulant.
References Greenblatt, E.N., et al.: J. Pharmacol. Exp. Ther., 131, 115 (1961), Padmanabhan, G.R., Anal. Profiles Drug Subs., 10, 473 (1981), Srinivas, N.R., et al.: Pharm. Res., 10, 14 (1993),

Stability Hygroscopic
Applications Desfuroyl Ceftiofur Dimer is an impurity of the drug Ceftiofur (C244695), a third generation cephalosporin antibiotic used in veterinary medicine.
References Donaldson, S.C. et al.: Appl. Environ. Microbiol., 72, 3940 (2006); Yancey, R.J. et al.: Am. J. Vet. Res., 48, 1050 (1987);

Applications Labelled Ursodeoxycholic Acid (U850000) derivative. 24-norUrsodeoxycholic acid is superior to Ursodeoxycholic acid in the treatment of sclerosing cholangitis in Mdr2 (Abcb4) knockout mice.
References Seedorf, U., et al.: J. Biol. Chem., 269, 21277 (1994), Stolowich, N., et al.: Biochemistry, 36, 1719 (1997),