Angiogenèse

<p>EGFR-IN-146 is an EGFR inhibitor that suppresses the EGFR signaling pathway and improves insulin sensitivity by activating the AMPK pathway. It effectively reduces blood glucose levels and body weight, showing great potential in the study of diabetes and obesity.</p>

<p>MTX-216 is an ATP-competitive inhibitor targeting both PI3K and EGFR. It simultaneously inhibits Ki-67 and ribosomal S6 phosphorylation, inducing apoptosis in NF1LOF cells. Additionally, MTX-216 suppresses SYK kinase activity with an IC50 of 281 nM. This compound is applicable for melanoma research.</p>

<p>FLT3/ITD-IN-1 inhibits FLT3-ITD with IC50s: 38.2 nM (FLT3) and 144.1 nM (ITD), and fights acute myeloid leukemia.</p>

<p>Tyk2-IN-3 is an inhibitor of Tyk2 pseudokinase (IC50: 485 nM).</p>

<p>(-)-Cevimeline HCl hemihydrate, a muscarinic agonist, treats Sjogren's xerostomia. Quick absorption, species-dependent metabolism.</p>

<p>EGFR-IN-38: low-toxic acrylamide-derived EGFR inhibitor, targets NSCLC, patented for research on EGFR mutation-related diseases.</p>

<p>Flonoltinib maleate is an orally active dual inhibitor of JAK2/FLT3, with IC50 values of 0.7 nM for JAK2, 4 nM for FLT3, 26 nM for JAK1, and 39 nM for JAK3. It exhibits anticancer properties.</p>

<p>JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active inhibitor of EGFR with an IC 50 of 15 nM for EGFR L858R/T790M [1].</p>

Ki11502 is a multi-target receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGFβ/α receptors (with an IC50 of less than 10 nM). It specifically suppresses PDGFβ receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Additionally, Ki11502 induces apoptosis and exhibits significant antiproliferative effects against specific leukemia subgroups, including those with Imatinib-resistant mutations. It is particularly suitable for studying the role of PDGF in vascular diseases and the involvement of proteoglycans in atherosclerosis.

<p>Lazertinib (mesylate) (YH25448 (mesylate); GNS-1480 (mesylate)) is an orally active EGFR inhibitor capable of crossing the blood-brain barrier. It suppresses the p-EGFR, p-AKT, and p-ERK signaling pathways, leading to apoptosis. Lazertinib (mesylate) demonstrates antitumor activity in the H1975-luc BM xenograft model in mice and is applicable for researching non-small cell lung cancer.</p>

<p>PNU-145156E is a noncytotoxic molecule inhibiting growth and angiogenic factors, suppress tumor angiogenesis, support anti-angiogenic research strategies.</p>

<p>TX2-121-1 targets HER3 for proteasome-mediated degradation to inhibit HER3-dependent signalling and growth.</p>

<p>Tyk2-IN-17 (compound 185) effectively inhibits TYK2 [1].</p>

<p>JAK1/TYK2-IN-4 serves as a dual inhibitor targeting both JAK and TYK2, displaying IC50 values of 39 nM and 21 nM, respectively. It is also orally bioavailable [1].</p>

Tyk2-IN-14, a small molecule inhibitor of TYK2, is significant in treating inflammatory diseases and conditions linked to hypersecretion of IFNa and interferons [1].

<p>NDI-034858 (TAK-279) is a tyrosine kinase 2 (TYK2) inhibitor (Kd&lt;200 pM) that targets the JH2 structural domain of Tyk2 for the treatment of autoimmune diseases</p>

JAK2-IN-7 selectively inhibits JAK2 (IC50: 3 nM), shows 14-fold selectivity over JAK1/3, FLT3, induces G0/G1 arrest, apoptosis, and has antitumor effects.

<p>XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that regulates protein kinases.</p>

<p>JDTic, a 4-phenylpiperidine derivative distantly related to analgesics like meperidine and ketobemidone and more closely to the mu opioid antagonist alvimopan, exhibits a notably long duration of action, maintaining effects in animals for weeks following a single dose. This duration is not due to irreversible binding to the kappa opioid receptor but rather to altered activity of c-Jun N-terminal kinases. As a highly selective antagonist for the κ-opioid receptor, without influencing the μ- or δ-opioid receptors, JDTic has shown potential in animal studies for producing antidepressant and anxiolytic effects. It also demonstrates promise in treating addiction to substances such as cocaine and morphine, distinguishing itself structurally from other kappa antagonists like norbinaltorphimine.</p>

Ibrutinib is a selective, irreversible Btk inhibitor (IC50: 0.5 nM). Ibrutinib Racemate is the racemate of Ibrutinib.

<p>ENMD-2076 is an orally active kinase inhibitor. It also has antiangiogenic and antiproliferative mechanisms of action.</p>

<p>Nimotuzumab (powder) is a humanized IgG1 monoclonal antibody that specifically targets the epidermal growth factor receptor (EGFR), possessing a dissociation constant (KD) of 0.21 nM. It blocks the binding to its ligand by targeting the extracellular domain of EGFR. Nimotuzumab exhibits strong antitumor activity by inducing both antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC), exerting cytolytic effects on target tumors.</p>

<p>PCI 45227 is an active metabolite of the Bruton's tyrosine kinase inhibitor ibrutinib .1PCI 45227 is formed from ibrutinib by the cytochrome P450 (CYP) isoform CYP3A.<br>1.Veeraraghavan, S., Viswanadha, S., Thappali, S., et al.Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: Application to a pharmacokinetic studyJ. Pharm. Biomed. Anal.107151-158(2015)</p>

<p>XMU-MP-3 is a robust, non-covalent inhibitor of BTK, exhibiting exceptional potency with IC50 values of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation, respectively, in the presence of 10 μM ATP. Moreover, XMU-MP-3 elicits apoptosis.</p>

<p>Tyrosine-protein kinase ABL, IC50: 1500 nM</p>

<p>(3R,4S)-Tofacitinib, the less active enantiomer of Tofacitinib, is a JAK3 inhibitor with an IC50 of 1 nM.</p>

<p>HMBD-001 is a humanized IgG1 monoclonal antibody inhibitor that targets HER3. By inhibiting the dimerization of HER3, HMBD-001 suppresses the growth and proliferation of tumor cells. It holds potential for research in cancer treatments, specifically for pancreatic cancer and non-small cell lung cancer.</p>

<p>PM-8002 is a bispecific antibody that targets PD-L1 and VEGF-A. It is applicable for research on solid tumors.</p>

<p>Desidustat is an inhibitor of HIF hydroxylase.</p>

<p>Duligotuzumab (MEHD-7945A) is a bispecific humanised IgG-κ monoclonal antibody targeting HER3 and EGFR, solid tumours, head and neck cancer,colorectal cancer.</p>

<p>Applications 3,3',4,4'-Tetrabromobiphenyl is multi-persistent organic pollutants analyzed in breast milk of first time mothers. An environmental pollutant that affects copper and molybdenum metabolism in rats. Also, it is derived from 1-Bromo-2- nitrobenze (B686175), which is an organic building block used for the synthesis of various pharmaceutical compounds. It is an intermediate for the synthesis of novel Diarylamino-1,3,5-triazine derivatives as FAK inhibitors with anti-angiogenic activity.<br>References Tlustos, C., et al.: Organohalogen Compd., 75, 1185-1188 (2013); Salman, K. N., et al.: Environ. Sci. Pollut. R., 21, 6400-6409 (2014); Dao, P., et al.: Bioorg. Med. Chem. Lett., 23, 4552 (2013);<br></p>

<p>KBP-7018: potent tyrosine kinase inhibitor targeting c-KIT, RET, PDGFR with IC50s of 10, 7.6, 25nM.</p>

<p>VEGFR inhibitor</p>