Angiogenèse

Applications AZ 5104 is a derivative of AZD 9291 (A808075) is a selective EGFR inhibitor (epidermal growth factor receptor), used in the treatments of nonsmall-cell lung cancer (NSCLC).
References Finlay, M.R.V., et al.: J. Med. Chem., 57, 8249 (2014);

Applications Tyrphostin AG 112 is an EGFR inhibitor.

Applications Atrasentan is a selective antagonist of the endothelin-A (ETA) receptor and binds selectively to the ETA receptor, which may result in inhibition of endothelin-induced angiogenesis and tumor cell proliferation.
References Bax, W., et al.: Trends Pharmacol. Sci., 15, 379 (1994); Winn, M., et al.: J. Med. Chem., 39, 1039 (1996); Wu-Wong, J., et al.: J. Pharmacol. Exp. Ther., 281, 791 (1997);

Applications 6-Amino-4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-7-ethoxyquinoline-3-carbonitrile, is used in the synthetic preparation of aminopropanamides which is used in irreversible inhibition of epidermal growth factor receptor (EGFR) for potential use in cancer therapy.
References Carmi, C., et al.: J. Med. Chem., 55, 2251 (2012)

Stability Moisture Sensitive
Applications 2,3-Naphthalic anhydride is used as a reagent to synthesize analogues of Thalidomide (T338850), an inhibitor of tumour necrosis factor that was once abandoned because it caused birth defects, but is currently used as an inhibitor of angiogenesis in patients with multiple myeloma.
References D’Amato, R., et al.: Proc. Nat. Acad. Sci., 91, 4082 (1994); Ehrenpreis, E., et al.: Gastroenterology, 117, 1271 (1999); Parma, T., et al.: Nat. Med., 5, 582 (1999); Singhal, S., et al.: New Engl. J. Med., 341, 1565 (1999)

Stability Hygroscopic
Applications Dihydrochloride salt of trans-3-Hydroxy Apatinib, a metabolite of the antiangiogenic agent and selective VEGFR2 inhibitor Apatinib (A726150).
References Ding, J, et al.: J. Chrom B Anal. Technol. Biomed. Life Sci., 895, 108 (2012);

Applications 4-Fmoc-3(R)-morpholinecarboxylic Acid is used to prepare 125I-labeled morpholine-containing RGD ligand of αvβ3 integrin as angiogenesis imaging probe.
References Bianchini, F., et al.: J. Med. Chem., 55, 5024 (2012)

Applications Tyrphostin AG 1478 is a potent and selective inhibitor of EGFR.

Applications 2-Chloro-N-[4-(1-cyanocyclopentyl)phenyl]-3-pyridinecarboxamide is an intermediate Apatinib 25-N-Oxide (A726160), a metabolite of the antiangiogenic agent and selective VEGFR2 inhibitor Apatinib (A726150).

Applications N4-​(2,​3-​Dimethyl-​2H-​indazol-​6-​yl)​-​N4-​methyl-2,​4-​pyrimidinediamine is a degredation product of Pazopanib (P210925), an oral angiogenesis inhibitor targeting VEGFR and PDGFR.
References Olaussen, K., et al.: Oncogen., 28, 4249 (2009), Sleijfer, S., et al.: J. Clin. Oncol., 27, 3126 (2009), Chan, A., et al.: Drugs, 69, 167 (2009), Patel, P. et al.: J. Mass. Spec., 50, 918 (2015);

QL-X-138: Dual BTK/MNK inhibitor; covalent to BTK, IC50=9.4 nM; non-covalent to MNK1/2, IC50=107.4/26 nM; dengue virus 2 IC50=3.5 μM; for B-cell malignancies.