Angiogenèse

<p>W23-1006 is a selective covalent ALKBH5 inhibitor. It binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. The inhibitory activity of W23-1006 is approximately 30 times stronger than that of FTO and 8 times greater than that of ALKBH3. W23-1006 is applicable for research in triple-negative breast cancer (TNBC).</p>

<p>EGFR-IN-23, identified as compound 8 in WO2021244502A1, is a potent EGFR tyrosine kinase inhibitor (TKI) demonstrating an inhibitory concentration (IC50) of 8.</p>

<p>JBJ-09-063: EGFR inhibitor, IC50s 0.147-0.396 nM for various mutants; hinders EGFR/Akt/ERK1/2 phosphorylation; targets TKI-sensitive/resistant lung cancer.</p>

<p>FAK-IN-26 is a blood-brain barrier-penetrating inhibitor of Focal Adhesion Kinase (FAK) with an IC50 of 0.87 nM. It significantly reduces tumor cell viability, cancer stem cell activity, and cell migration in A549 and SKOV-3 cell lines. FAK-IN-26 exhibits potent anticancer activity, achieving tumor inhibition rates of 59.15% and 57.9% in A549 and SKOV-3 tumor mouse models, respectively.</p>

<p>EGFR-IN-139 (compound PD 18) is an EGFR inhibitor with IC50 values of 12.88 nM (wild type), 10.84 nM (L858R/T790M), and 42.68 nM (L858R/T790M/C797S). It demonstrates significant anticancer activity against the A549 and H1975 cancer cell lines, which express high levels of EGFR. EGFR-IN-139 exhibits strong selectivity for cancer cells and can be utilized in research on non-small cell lung cancer (NSCLC).</p>

<p>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.</p>

<p>FLT3-IN-13 inhibits topoisomerase II/FLT3 in leukemia with IC50 of 2.26 μM, causes G2/M arrest, and promotes apoptosis.</p>

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

<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>

<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>

<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>

<p>Ibrutinib is a selective, irreversible Btk inhibitor (IC50: 0.5 nM). Ibrutinib Racemate is the racemate of Ibrutinib.</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>Tyrosine-protein kinase ABL, IC50: 1500 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>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>ENMD-2076 is an orally active kinase inhibitor. It also has antiangiogenic and antiproliferative mechanisms of action.</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>(3R,4S)-Tofacitinib, the less active enantiomer of Tofacitinib, is a JAK3 inhibitor with an IC50 of 1 nM.</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>VEGFR inhibitor</p>