Angiogenesis

Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of

Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells,antitumor and antileukemic.

Stability Hygroscopic Applications 5-Amino-2-methylbenzenesulfonamide is an intermediate for the synthesis of Pazopanib (P210925), an oral angiogenesis inhibitor targeting VEGFR and PDGFR. References Harris, P.A., et al.: J. Med. Chem., 51, 4632 (2008); Petrow, V., et al.: J. Pharmacy. Pharmacol., 12, 705 (1960);

HIF-2α-IN-3 is an allosteric inhibitor of HIF-2α (IC50: 0.4 μM; KD: 1.1 μM) with anticancer activity.

THS-044 (N-[2-Nitro-4-(Trifluoromethyl)phenyl]morpholin-4-Amine) binding stabilizes the HIF2α PAS-B folded state with a kd of 2 μM and regulates HIF2 activity

Applications N-(4-Chloro-2-pyrimidinyl)-N,2,3-trimethyl-2H-indazol-6-amine is an intermediate in the synthesis of 5-((2-((2,3-Dimethyl-2H-indazol-6-yl)(methyl)amino)pyrimidin-4-yl)amino)-2-methylbenzenesulfonamide Hydrochloride (D474433) which is an impurity of Pazopanib (P210925), which 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),

EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-231 and MDA-MB-435 cells, equally effective inhibition for Rac3.

HIF-1α-IN-2 is a HIF-1α inhibitor with anticancer activity that inhibits the expression of HIF-1α and VEGF, and inhibits cell migration.

FGFRs-IN-1 (Compound A16) is an orally active inhibitor targeting FGFR1/2/3/4, with IC50 values of 2.3, 7, 11, and 163 nM respectively. It also inhibits VEGFR1/2/3, Abl, and Flt3, with IC50 values of 61, 176, 112, 26, and 353 nM. The compound shows weak inhibition of CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and it inhibits epithelial-mesenchymal transition (EMT) in A549 cells stimulated by TGF-β1. Additionally, FGFRs-IN-1 demonstrates anti-inflammatory activity in mouse models of lung fibrosis induced by Bleomycin and liver fibrosis induced by CCl4.

Applications tert-Butyl (2,6-Dioxopiperidin-3-yl)carbamate is an intermediate in the synthesis of Thalidomide-d4 (T338852), a labelled Thalidomide, which inhibits FGF-induced angiogenesis. Inhibits replication of human immunodeficiency virus type 1. Teratogenic sedative. References D’Amato, r.J., et al.: Proc. Natl. Acad. Sci. USA, 91, 4082 (1994); Makonkawkeyoon, S., et al.: Proc. Natl. Acad. Sci. USA, 90, 5974 (1993); Schumacher, H., et al.: J. Pharmacol. Exp. Therap., 160, 189 (1968)

AG1557 (AG-1557) is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194).

Tyrosine kinase-IN-9 (Compound B) is an inhibitor of c-Abl. It is useful for studying neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease.

TZEP7 functions as an EGFR kinase inhibitor in cancer cells. It exhibits cytotoxicity and induces apoptosis within these cells. TZEP7 downregulates the anti-apoptotic protein Bcl-2, upregulates the pro-apoptotic protein Bax, and increases caspase levels. This compound holds potential for research in anticancer drug development.

Endoxifen Z-isomer (EDX) is a key active metabolite of tamoxifen with higher affinity and specificity to estrogen receptors that inhibits aromatase activity.

Applications (1S,3S)-3-((tert-Butyldimethylsilyl)oxy)-1-(4-nitrophenyl)cyclopentanecarboxamide is an impurity in the synthesis of metabolites of the antiangiogenic agent and selective VEGFR2 inhibitor Apatinib (A726150).

CAIX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. It exhibits anticancer activity by inhibiting the growth of MCF-7 breast cancer cells (IC50 of 22.33 μM) and mouse fibroblast cell line 3T3, where cell viability is reduced to below 40% at a concentration of 100 μM. This compound is applicable for research in the field of cancer treatment.

EGFR-TK-IN-5 (Compound NCE 2) is a thiazolyl pyrazoline derivative with significant inhibitory activity and stability against EGFR. It is applicable in tumor research.

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);

EGFR-IN-147 (compound ID-5841161) is a potent EGFR inhibitor, demonstrating a 14% inhibition rate at a concentration of 1μM. It holds promise for cancer research applications.

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM).

Applications Pulsatilla Saponin D shows antiangiogenic and antitumor activity. References Sang-Won, H. et al.: Carcinogen., 34, 2156 (2013);

VEGFR-2-IN-65 (Compound 07) functions as a VEGFR-2 inhibitor. It forms hydrogen bonds with Cys180 and can inhibit tube formation in HUVECs.

Applications α-Eudesmol is an isomer of β-Eudesmol (E938600), a sesquiterpenoid known to induce neurite outgrowth. β-Eudesmol exhibits antiangiogenic activity. References Obara, Y. et al.: J. Pharmacol. Exp . Ther., 30, 803 (2011); Tsuneki, H. et al.: Eur. J. Pharmacol., 512, 105 (2005);

HIF-2α-IN-1 is a potent HIF-2α inhibitor with IC50 values less than 500 nM.

HA 155 (Autotaxin Inhibitor IV) is a boronic acid-based compound, inhibiting ATX with IC50 of 5.7 nM by selectively binding to its catalytic threonine.

FAK-IN-24 (Compound 9f) is a potent FAK inhibitor with an IC50 of 0.815 nM. It induces DNA damage and apoptosis, and exhibits activity against glioblastoma. FAK-IN-24 effectively inhibits proliferation of glioblastoma cell lines U87-MG (IC50= 15 nM) and U251 (IC50= 20 nM), and suppresses tumor growth in U87-MG xenograft models.

KIT/PDGFRA-IN-1 (compound 19) is an inhibitor targeting the stem cell growth factor receptor (KIT) and platelet-derived growth factor receptor alpha (PDGFRA). Its IC50 values are 2.3 µM for KIT-wt, 12 µM for KIT-D816H, 492 µM for KIT-T670I, 0.8 µM for PDGFRA-wt, 99.9 µM for PDGFRA-D842V, 42.3 µM for PDGFRA-T674I, and 4.3 µM for PDGFRA-G680R. The GR50 values for GIST-T1, T1-a-D842V, and GIST-48B cell lines (gastrointestinal stromal tumor cell lines with PDGFR and KIT mutations) are 12 nM, 8900 nM, and ≥10,000 nM, respectively.

ABP-102 (CT P72) is a bispecific t-cell adduct (BiTE) that acts as a CD3 modulator and selective HER2 modulator for targeting HER2 overexpressing tumors.

Applications Methylhydroquinone is a marine fungus metabolite, showing activity as an angiosupressor that interferes with the Akt pathway. Allows for screening of novel inhibitors of angiogenesis. References Garcia-Caballero, M. et al.: Biochem. Pharm., 85, 1727 (2013);

Applications It is an alkaloid isolated from Radix et Rhizoma Leonticis. It shows various pharmaceutical properties: bacteriostatic, wound healing, cytotoxicity, immunosuppression, acetilcholinesterase inhibition, and inhibition of the activity of tumor angiogenesis. References Perdue, G.P., et al.: J. Pharm. Sci., 68, 124 (1979), Tsacheva, I., et al.: J. Biosci., 59, 528 (2004), Zhang, Y., et al.: Cancer Lett., 262 103 (2008),

DA-0157 is an orally active inhibitor targeting EGFR and ALK, designed to overcome resistance mutations in non-small cell lung cancer (NSCLC). It effectively inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50= 6.9 nM), Ba/F3-EGFR WT (IC50= 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50= 5.5 nM), and Ba/F3-EML4-ALK (IC50= 7.4 nM). Additionally, DA-0157 inhibits CYP2D6 with an IC50 of 5.26 μM and demonstrates antitumor activity in mouse models.

Applications N-(4-((1R,3R)-3-((tert-Butyldimethylsilyl)oxy)-1-cyanocyclopentyl)phenyl)-2-chloronicotinamide is an impurity in the synthesis of metabolites of the antiangiogenic agent and selective VEGFR2 inhibitor Apatinib (A726150).

IBI-334 is a bispecific antibody targeting both B7-H3 and EGFR. It features an EGFR arm responsible for signal blocking, connected to a modified B7-H3 arm that ensures optimal affinity and binding. The antibody is afucosylated to enhance its antibody-dependent cellular cytotoxicity (ADCC) effects. IBI-334 is widely applicable in EGFR-driven solid tumors.

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)

Applications Glycerol 1-Monobutyrate functions as a key regulatory molecule in angiogenic process. References Dobson, D. E., et al.: Cell (Cambridge, MA, U. S.), 61, 223 (1990)

Applications Methyl 2,​5-​Dihydroxybenzoate is a general reagent used in the synthesis of angiogenesis inhibitors that display anti-tumor activity. References Marin-Ramos, N. et al.: J. Med. Chem, 58, 3757 (2015);

Applications 2-Acetylnaphthalene is an intermediate used to prepare piperidinyl pyrazoles as potent DNA gyrase inhibitors It is also used in the synthesis of aromatic enone and dienone analogues of curcumin as angiogenesis inhibitors. References Tanitame, A., et al.: J. Med. Chem., 47, 3693 (2004); Robinson, T., et al.: Bioog. Med. Chem. Lett., 13, 115 (2003)

TrxR/EGFR-IN-1 (Compound L1Au2) is a TrxR/EGFR inhibitor with activity against both gefitinib-sensitive and -resistant lung cancer, effectively suppressing tumor proliferation and promoting apoptosis. It enhances GPX4 degradation through autophagosome-lysosome and proteasome pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it applicable for studies on gefitinib-resistant lung cancer.

Stability Light Sensitive Applications Fumagillin is a compound isolated from the fungus Aspergillus fumigatus. Fumagillin is an antimicrobial agent used in the treatment of microsporidiosis. Fumagillin shows promise as both an an anti-infective and antiangiogenic agent. References Molina, J.M. et al.: N. Eng. J. Med., 346, 1963 (2002); Hou, L. et al.: Pathol. Int., 59, 448 (2009); Ingber, D. et al.: Nature, 348, 555 (1990);

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 Pazopanib-d3 is the isotope labelled analog 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),

PROTAC FGFR1 degrader-1 (compound S2H) is a targeted degrader of FGFR1, demonstrating an IC50 of 26.81 nM and a DC50 of 39.78 nM in KG1a cells. This compound is composed of a CRBN-type E3 ligase ligand (blue part) Pomalidomide, a target protein ligand (red part) FGFR1ligand-1, and a PROTAC linker (black part) 9-Bromononanoic acid, together forming the conjugate E3LigaseLigand-linker Conjugate 164.

Applications N-(4-Chloro-2-pyrimidinyl)-2,3-dimethyl-2H-indazol-6-amine is an intermediate in the synthesis of 5-((2-((2,3-Dimethyl-2H-indazol-6-yl)(methyl)amino)pyrimidin-4-yl)amino)-2-methylbenzenesulfonamide Hydrochloride (D474433) which is an impurity of Pazopanib (P210925), which 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),

Protein kinase inhibitor 10 is a protein kinase inhibitor with IC50 values of 28.9 μM, 13.6 μM, and 2.41 μM for TAM receptors, FAK, and KIT, respectively. It can inhibit abnormal and excessive cell proliferation, showing potential for research in the field of cancer treatment.

Tivozanib (KRN951) is an oral VEGFRs 1-3 inhibitor with potential antiangiogenic and cancer-fighting properties.

Cavutilide has antiarrhythmic activity, inhibits hERG K(+) channels, and can be used to study heart failure and persistent atrial fibrillation.

FM19G11 is an inhibitor of hypoxia inducible factor (HIF) α-subunit (IC50 = 80 nM in hypoxia induced luciferase assay).

Acriflavine HCl is a HIF-1α inhibitor reducing PGK1, VEGF, and HIF-1α levels both in vitro and in vivo.

Applications The Hydrochloride salt of Pazopanib (P210925) a oral angiogenesis inhibitor targeting VEGFR and PDGFR. References Sleijfer, S., et al.: J. Clin. Oncol., 27, 3126 (2009), Chan, A., et al.: Drugs, 69, 167 (2009),

Applications Labelled Apatinib 25-N-Oxide (A726160). 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);

CGP062464 is an inhibitor of the tyrosine kinase c-Src, with an IC50 of less than 50 nM. It is utilized in research related to osteoporosis and tumor-induced hypercalcemia.

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6

Lirucitinib is a JAK inhibitor known for its anti-inflammatory properties.

Hck-IN-2 (Compound 8e) acts as an HCK inhibitor with demonstrated cytotoxic effects on tumor cells. It exhibits an IC50 of 19.58 μM for MDA-MB231 cells and 1.42 μM for MCF-7 cells. Additionally, Hck-IN-2 possesses antitumor activity.

Applications Bisphenol Z-d6 is the isotope labelled analog of Bisphenol Z. Bisphenol Z is one of the many derivatives of Bisphenol A (B519495) that can be used as HIF (hypoxia-inducible factor) inhibitors, antitumor agents, angiogenesis inhibitors, and antihypoxic agents. References Imaoka, S., Bisphenol A derivatives as HIF inhibitors. Jpn. Kokai Tokkyo Koho. JP 2011195574 A 20111006. Oct 6, 2011

Applications A potent, selective, cell permeable histone deacetylase inhibitor (HDAC). Displays anti-angiogenic activity by interfering with VEGF signaling in human umbilical vein endothelial cells (HUVECs). Induces differentiation in uman breast cancer cells. References Richon, V.M., et al.: Proc. Natl. Acad.Sci. USA, 95, 3003 (1988), Munster, P.N., et al.: Cancer Res., 61, 8492 (2001), Deroanne, C.F., et al.: Oncogene, 21, 247 (2002),

Applications 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),

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);

Glesatinib, an oral tyrosine kinase inhibitor, targets c-Met and VEGFR2 with IC50s of 29 nM and 10 nM, may treat cancer.

EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR/COX-2-IN-1 significantly increases the proportion of cells in the G2/M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.

Applications 1-(Phenylmethyl)-4-piperidinamine is used in the preparation of 4-substituted coumarins as novel acetylcholinesterase inhibitors used in the treatment and various therapeutic approaches to Alzheimer’s disease. It is also used in the synthesis of nicotinamide derivatives as anti-angiogenic agents. References Razavi, S. et al.: Eur. J. Med. Chem., 64, 252 (2013); Choi, H. et al.: Bioorg. Med. Chem. Lett., 23, 2083 (2013);

Stability Hygroscopic Applications The hydrochloride salt of AZ 5104 (A795170), which is a derivative of AZD 9291 (A808075) and 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);

HER2-IN-21 (compound 657994) is an inhibitor of the human epidermal growth factor receptor 2 (HER2) with an IC50 value of 3.85 μM.

M1002, a HIF-2 agonist, boosts HIF-2alpha/ARNT activation and alters HIF-281alpha PAS-B, working with PHD inhibitors.