Angiogenèse

<p>Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.</p>

<p>FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor properties. It selectively targets cancer cells with FLT3 internal tandem duplication (ITD) mutations, demonstrating IC50 values of 85, 290, 130, 65, and 220 nM against BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively. These lines include acute myeloid leukemia (AML) cells harboring FLT3-ITD mutations such as MV4-11 and MOLM-13/14. The compound also reduces phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells, leading to cell cycle arrest and apoptosis. With an oral bioavailability of 19.2% in SD rats, FLT3-IN-28 extends survival in a dose-dependent manner in MOLM-13 xenografted NSG mouse models. It holds promise for research in FLT3-ITD-related cancer studies.</p>

<p>PEPvIII, a peptide sequence from EGFRvIII, was designed to represent a target of glioma and is presented by MHC I/II complexes.</p>

<p>HER2-IN-14 (Compound 34) is a potent inhibitor of HER2, achieving an inhibitory concentration (IC50) of 18 nM.</p>

<p>Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.</p>

<p>ML 2-23 is a potent BCR-ABL degrader operating as a PROTAC, exhibiting selective proteasome-dependent degradation of BCR-ABL within leukemia cells [1].</p>

<p>IMS2186: antichoroidal neovascularization reagent, arrests G2/M cancer phase, anti-proliferative, reduces eye leakage, non-toxic.</p>

<p>EGFRT790M/L858R-IN-9 (Compound 8) is an inhibitor targeting the EGFR-L858R/T790M mutations. It effectively inhibits the phosphorylation of the EGFR-L858R/T790M mutant kinase, demonstrating an IC50 value of 0.0064 µM. Additionally, EGFRT790M/L858R-IN-9 can suppress the proliferation of non-small cell lung cancer (NSCLC) cells, making it useful for cancer research.</p>

<p>HIF-1 inhibitor-4 (HIF-1 inhibitor-4) is a HIF-1 inhibitor with IC50 of 560 nM.</p>

<p>SA-VA, an intracellular self-assembled PROTAC featuring azide and alkyne groups, selectively degrades VEGFR-2 and EphB4 proteins within U87 cells.</p>

<p>Zilurgisertib (INCB-000928) is a selective and potent ALK 2 inhibitor for the study of cancer and MF anemia.</p>

<p>EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively.</p>

<p>Mersalyl is an organic mercurial diuretic.</p>

<p>HAT-SIL-TG-1&amp;AT: a hypoxia-activated JAK inhibitor that curbs HEL cell growth &amp; STAT3/5 phosphorylation in tumors.</p>

<p>AMX-818 is a conditionally activated, masked T cell engager (TCE) that targets HER2. It demonstrates potent T cell cytotoxicity against HER2-positive tumor cell lines and can induce tumor regression in vivo. AMX-818 holds promise for research into HER2-positive solid tumors.</p>

<p>IOX2-NH2-Methyl is a modified form of IOX2. IOX2 is a specific inhibitor of PHD2 (prolyl-hydroxylase-2), capable of upregulating HIF-1α expression and suppressing ROS production. IOX2-NH2-Methyl is employed in investigations of platelet and thrombus formation.</p>

<p>AG1478 HCl is an epidermal growth factor receptor protein inhibitor.</p>

<p>Sunitinib D10, a deuterium-enriched version, inhibits VEGFR2 and PDGFRβ tyrosine kinases (IC50: 80 nM/2 nM).</p>

<p>Asciminib (ABL001) hydrochloride is a selective and potent mutant BCR-ABL1 inhibitor that inhibits Ba/F3 cell growth (IC50: 0.25 nM).</p>

<p>Nilotinib D6 is a deuterium labeled Nilotinib which is an orally available inhibitor of Bcr-Abl tyrosine kinase ,and with antineoplastic activity.</p>