Angiogenesis

Applications An oral, irreversible dual EGFR/HER2 inhibitor for breast and non-small cell lung cancer. Antitumor agent. References Vogel, C., et al.: J. Clin. Oncol., 20, 719 (2002), Ji, H., et al.: Cancer Cell., 9, 485 (2006), Sequist, L., et al.: Oncologist, 12, 325 (2007),

JAK1/STAT3-IN-1 (compound 4f) functions as an anti-atopic dermatitis (AD) agent by inhibiting the JAK1/STAT3 signaling pathway. It has an IC50 value of 2.17 μM for inhibiting NO production. Additionally, JAK1/STAT3-IN-1 improves skin conditions in AD-like mice by reducing inflammatory infiltration, suppressing the expression of p-JAK1/JAK1 and p-STAT3/STAT3, and alleviating the hyperimmune response induced by MC903 (Calcipotriol).

(Rac)-PT2399 is a potent and specific inhibitor of hypoxia-inducible factor 2a (HIF-2α)(IC50 of 0.01 μM).

HIF1-IN-3 (Benzenepropanamide, N-[(8-hydroxy-7-quinolinyl)(4-methoxyphenyl)methyl]-) is an effective inhibitor of HIF-1 (EC50 = 0.9 μM) and can be used in

Applications N2,N4-bis(2,3-dimethyl-2Hindazol-6-yl)-2,4-pyrimidinediamine Hydrochloride is a Pazopanib (P210925) dimer impurity. Pazopanib is 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); Li, Y. et al.: J. Pharm. Biomed. Anal., 52, 493 (2010);

Applications 1,1-(Ethylenedioxy)-3-bromopropane is used in the synthesis of EGFR inhibitors. Also used in the synthesis of orally active agents of cancer and cell proliferation with quinoline substructures. References Zhang, X. et al.: Arch. Pharm., 346, 44 (2013); Lee, Y. et al.: J. Med. Chem., 55, 10363 (2012);

VEGFR/PDGFR-IN-1 (Compound 1) is an inhibitor of VEGFR with an IC50 of 0.4 μM. It can inhibit angiogenesis in HUVEC cells and holds promise for impeding tumor growth and metastasis.

FGFR1inhibitor-17 (Compound 92) is a potent inhibitor of FGFR1, with promising applications in cancer research.

Applications Apatinib 25-N-Oxide is 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);

Impurity Phenazone EP Impurity A Applications Edaravone inhibits the disease activity in rheumatoid arthritis. Edaravone can significantly enhance IR flap viability and protect flap vessels, which is related to scavenging oxygen free radicals, reducing the consumption of SOD, reducing the extent of lipid peroxidation and inflammation, and protecting functional structure of vessels in the early stages of reperfusion. It also shows protective effects against STZ-induced cognitive impairment, oxidative stress, cholinergic dysfunction and altered protein expressions. Its acts like a free radical scavenger, decreased apoptotic cell death, oxidative damage to DNA and lipids, and angiogenesis through inhibiting JNK and p38 MAPK pathways in AMD, glaucoma, DR, and RVO animal models. References Reeta KH et al. Eur J Neurosci. 2017 Feb 15Masuda T et al. Oxid Med Cell Longev. 2017;2017:9208489Zhang DY et al. J Huazhong Univ Sci Technolog Med Sci. 2017 Feb;37(1):51-56Criswell LA et al. Am J Med. 2002 Apr 15;112(6):465-71.

Impurity Ketoprofen EP Impurity B Applications Desmethyl Ketoprofen (Ketoprofen EP Impurity B) shows antiinflammatory and analgesic activities. It can be used as neoplasm inhibitors and for treatment of angiogenesis-related disorders. References Allais, A., et al.: Eur. J. Med. Chem., 9, 381 (1974).

Applications Xanthohumol is found in the hop plant Humulus Lupulus. Xanthohumol decreases inflammation, oxidative stress, and angiogenesis during the healing of skin wounds in type 1 diabetic rats. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Costa, R., et. al.: J. Nat. Prod., 76, 2047 (2013) Yuan, Y., et. al.: Eur. J. Pharmaceut. Sci., 53, 55 (2014)

Impurity Clopidogrel Impurity B; Clopidogrel USP B; Clopidogrel USP Related Compound B Applications Clopidogrel Related Compound B (Clopidogrel Impurity B; Clopidogrel USP B; Clopidogrel USP Related Compound B) is a tetrahydrothienopyridine as inhibitor of angiogenesis. References Maffrand, J. P., et al.: Eur. J. Med. Chem., 9, 483 (1974), Thebault, J.J., et al.: Clin. Pharmacol. Ther., 18, 485 (1975),

K882 (Compound 4e) is an Src inhibitor with a KD of 0.315 μM. It induces apoptosis and inhibits XIAP and Survivin. Additionally, K882 blocks the activation of the PI3K/Akt/mTOR, Jak1/Stat3, and Ras/MAPK signaling pathways. K882 exhibits antitumor activity against non-small cell lung cancer.

ENMD-119 is a 2-methoxyestradiol analog with antiproliferative and antiangiogenic activity. It is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.

Applications 2,5-Difluorobenzoic Acid acts as a reagent in the synthesis of rutaecarpine and analogs used for the removal of caffeine from the body. Prepparation of quinolone carboxylic acids as cell-permeable inhibitors of protein tyrosine phosphatase (Erratum). Preparation, molecular docking, and bioactivity of α-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis. Also used as new passive water tracers for oil field applications. References Liang, L., et al.: Tetrahedron Lett., 56, 2466 (2015); Zhi, Y., et al.: Bioorg. Med. Chem., 22, 4347 (2014); Serres-P, C., et al.: Energy & Fuels, 25, 4488 (2011); Chen, J., et al.: J. Med. Chem., 53, 4545 (2010)

Applications 2,3-Bis(4-(benzyloxy)-3-methoxyphenyl)propan-1-amine-d4 is an catecholamine based derivative with potential anti-angiogenic properties.

EGFR-IN-149 (Compound 3-OH) is an EGFR inhibitor with an IC50 value of 0.42 nM.

Applications A nitrosourea alkylating agent approved in Japan for the treatment of chronic myelogenous leukemia and polycythemia vera. It can be used in biological study of synthesis of anti-EGFR antibody-drug conjugates. It can also be used in therapeutic use and biological study of BCMA (B-Cell Maturation Antigen) antigen binding proteins. References Choi, H., et al.: PCT Int. Appl., WO 2017051254 A1 20170330 (2017);