Angiogenèse

<p>TYD-68 is a potent and selective CRBN-recruiting TYK2 PROTAC degrader, with a DC50 value of 0.42 nM. This compound effectively inhibits IL-12 and IFN-α-induced phosphorylation of STAT4 and STAT1, thereby blocking TYK2-dependent signaling pathways. TYD-68 is applicable in psoriasis research.</p>

<p>JH-XI-10-02 selectively degrades CDK8 (IC50: 159 nM) through proteasome, sparing CDK8 mRNA and CDK19.</p>

<p>Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ).</p>

<p>Potent PROTAC EGFR degrader 2; IC50: 4.0 nM, DC50: 36.51 nM; inhibits cell growth; for NTR-responsive synthesis.</p>

<p>MLK3-IN-1 (Compound 37) is a selective inhibitor of mixed-lineage kinase 3 (MLK3) with an IC50 of less than 1 nM. It also inhibits FAK with an IC50 of 15.5 μM. In both murine and human liver microsomes, MLK3-IN-1 demonstrates excellent metabolic stability.</p>

<p>Tomuzotuximab: fully human, glycoengineered IgG1 anti-EGFR monoclonal antibody with anticancer properties.</p>

<p>Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI) exhibiting antiproliferative activity against the chronic myeloid leukemia (CML) cell line K562, with a CC50 of 0.8 µM. Tyrosine kinase-IN-8 is applicable for research in chronic leukemia.</p>

<p>Apoptosisinducer 35 (Compound 6) is a multi-target inhibitor that reduces the expression of EGFR, AKT, ERK, and P38-MAPKα. It suppresses the proliferation of cancer cells A549 and Jurkat, induces cell cycle arrest at the S phase, and triggers apoptosis (cell death).</p>

<p>BV02 blocks 14-3-3 interactions, useful in chronic myeloid leukemia research, targets T315I mutant and wild-type Bcr-Abl cells.</p>

<p>Abicipar pegol is an anti-VEGF DARPin for ocular diseases, reducing retinal thickness and leakage.</p>

<p>MHES0488A is a selective humanized antibody targeting HER2, with a KD value of 0.8 nM. It constitutes the antibody portion of DHES0815A. Upon cellular internalization, MHES0488A is transported to lysosomes, releasing PBD-monoamide into the nucleus, where it alkylates DNA, inducing DNA damage and apoptosis. It shows potential for research in cancers such as HER2-positive breast cancer and gastric cancer.</p>

<p>Emavusertib (CA-4948) hydrochloride, a selective and potent IRAK4/FLT3 inhibitor, is designed for oral administration. It achieves an IC 50 of 57 nM against IRAK4 in a FRET kinase assay and demonstrates anti-tumor activity [1] [2] [3].</p>

<p>Syk-IN-4: potent, selective SYK inhibitor, orally bioavailable, IC50=0.31 nM, targets autoimmunity, cancers.</p>

<p>SNIPER(ABL)-058, a compound that links Imatinib (ABL inhibitor) with a derivative of LCL161 (IAP ligand) through a linker, effectively decreases BCR-ABL protein</p>

<p>AD57, a polypharmacological agent, blocks RET kinase (IC50: 2 nM), disrupts related kinases, and hinders cancerous activities like invasion and proliferation.</p>

<p>SJ988497: PROTAC JAK2 degrader, inhibits CRLF2r cell growth, degrades GSPT1, combines Ruxolitinib, linker, Pomalidomide; researched for ALL.</p>

<p>Multi-kinase-IN-5 (compound 15c) is a multi-kinase inhibitory agent that shows significant inhibition against a range of protein kinases including RET, KIT,</p>

<p>PROTAC BCR-ABL Degrader-1 (compound PROTAC 1), featuring a 2-oxoethyl linker, promotes Bcr-Abl degradation through the ubiquitin-proteasome pathway and</p>

<p>BMS-599626 2HCL (AC480 2HCl) is a BMS-599626 derivative.</p>

<p>FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor, demonstrating IC50 values of 1 nM for FLT3-D835Y and 4 nM for FLT3-ITD.</p>

<p>JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 ( IC 50 = 29 and 41 nM respectively).</p>

<p>Pacritinib (SB1518) citrate effectively inhibits wild-type JAK2 (IC 50 =23 nM) and the JAK2 V617F mutant (IC 50 =19 nM). It also targets FLT3 (IC 50 =22 nM) and the FLT3 D835Y mutant (IC 50 =6 nM). This compound is utilized in the study of acute myeloid leukemia (AML) and myelofibrosis (MF) [1] [2] [3].</p>

<p>Ibrutinib dimer is an impurity of Ibrutinib. IIbrutinib dimer is a Dimer of Ibrutinib. Ibrutinib is an irreversible Btk inhibitor (IC50: 0.5 nM).</p>

<p>SA-PA, a self-assembled intracellular PROTAC leveraging azide-alkyne click chemistry, selectively degrades VEGFR-2, PDGFR-β, and EphB4 proteins within U87 cells</p>

<p>(R)-3-Hydroxy Midostaurin: potent kinase inhibitor, major midostaurin metabolite via CYP3A4, potential AML treatment.</p>

<p>M4K2234 (26b) inhibits ALK2/ALK5 (IC50: 5/2144 nM), used as a probe for ALK1/2 kinases in cancer research.</p>

<p>PTD10, a highly potent PROTAC BTK degrader, exhibits a DC50 of 0.5 nM and a KD of 2.28 nM.</p>

<p>JBJ-09-063 TFA, an EGFR inhibitor selective for EGFR mutations, IC50s: 0.147-0.396 nM, blocks EGFR/Akt/ERK signaling, for EGFR-mutant lung cancer research.</p>

<p>Bevasiranib is a siRNA targeting VEGF production, key in choroidal neo-vascularization and wet AMD.</p>

<p>EGFR-IN-116 (compound 14D) is an antineoplastic agent. It exhibits an IC50 value of 0.103 μM for EGFR, 0.069 μM for VEGFR-2, and 19.74 μM for Topo II.</p>

<p>PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual inhibitor targeting PRMT5 and EGFR, with IC50 values of 15.47 μM and 19.31 μM, respectively. It demonstrates antiproliferative activity against the A549, MCF7, HeLa, and MDA-MB-231 cell lines. This compound also exhibits favorable pharmacokinetic (PK) and pharmacodynamic (PD) properties in vivo and significantly inhibits the growth of MCF7 orthotopic xenograft tumors.</p>

<p>SJF620 hydrochloride is a PROTAC that utilizes a lenalidomide analog to recruit CRBN and ligands to target Btk, exhibiting a DC50 of 7.9 nM [1].</p>

<p>A unique collection of 1353 proangiogenic and antiangiogenic compounds for new targets identification, research in mechanisms of angiogenesis, and high</p>

<p>HER2-IN-13 (Compound 33) serves as an effective HER2 inhibitor, exhibiting an IC50 value of 8 nM, and additionally demonstrates inhibition of wt-EGFR with an</p>

<p>EGFR/CDK2-IN-2 (compound 6a) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 19.6 nM and 87.9 nM, respectively.</p>

<p>PF15, a PROTAC for FLT3-ITD, degrades FLT3 kinase. DC50: 76.7 nM; hinders FLT3-ITD+ cell growth; potential in leukemia.</p>

<p>SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker.</p>

<p>VEGFR-2/InhA-IN-1, a dual inhibitor based on pyrazole, targets InhA and VEGFR, exhibiting both anti-tuberculosis and anti-angiogenic properties. It demonstrates effective antibacterial activity against the Mycobacterium tuberculosis H37Rv strain (MIC = 6.25 μg/mL) and significantly suppresses VEGFR-2 activity (IC 50 = 15.27 nM).</p>

<p>Compound 5K (Multi-target kinase inhibitor 2) is a multi-targeted kinase inhibitor demonstrating activity against EGFR, Her2, VEGFR2, and CDK2 with IC50 values</p>

<p>SNIPER(ABL)-019, a compound that links Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, exhibiting a</p>

<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>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.</p>

<p>Cisapride acts directly as a selective agonist of serotonin 5-HT4 receptor with IC50 value of 0.483 μM. And It also acts indirectly as a parasympathomimetic.</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>DSPE-PEG1000-GE11 is a PEG compound made up of DSPE and an EGFR-targeting peptide (GE11). GE11 is applicable for cancer cells overexpressing EGFR. DSPE-PEG1000-GE11 serves a role in drug delivery.</p>

<p>LH168 is a potent and selective probe for WDR5, with a SPR Kd value of 13 nM.</p>

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

<p>EGFR-IN-140 (Compound 31) is an inhibitor of EGFR, effectively targeting both wild-type EGFR and the EGFRL858R/T790M/C797S mutant, with Ki values of 0.95 nM and 2.1 nM, respectively. Additionally, it inhibits EGFRdel19/T790M/C797S in Ba/F3 cells with an IC50 of 56.9 nM and demonstrates antitumor activity in mouse models.</p>

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

<p>Efruxifermin, a modified FGF21 with IgG1 Fc, has increased stability and affinity. Used in non-alcoholic steatohepatitis research.</p>

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

<p>Vulinacimab (HLX-06) is a mAb targeting VEGFR-2, used in cancer research, vital for tumor angiogenesis and endothelial cell functions.</p>

<p>ALK-IN-9 effectively inhibits cell growth with IC50 &lt;0.2 nM for Ba/F3-EML4-ALK, KM12, KG-1.</p>

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

<p>Ilunocitinib is a non-selective and orally active Janus kinase (JAK) inhibitor for pruritus and atopic dermatitis caused by atopic dermatitis in dogs.</p>

<p>Tirbanibulin is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).</p>

<p>Tetrac (Tetraiodothyroacetic acid) is a derivative of L-thyroxine (T4), a thyroxine integrin receptor antagonist.Tetrac induces antiproliferation by blocking</p>

<p>(3S, 4S)-PF-06459988, a less active S enantiomer, specifically inhibits T790M mutant EGFR with high selectivity.</p>

<p>PND-1186 hydrochloride (VS-4718 hydrochloride) is a highly specific, reversible and potent inhibitor of FAK (IC50: 1.5 nM), which can selectively induce</p>

<p>Naphazoline nitrate: α1-adrenergic agonist, induces autophagy, necrosis in cancer cells, inhibits differentiation, treats congestion and eye issues.</p>

<p>FLT3-IN-16 is a potent FLT3 inhibitor (IC50 = 1.1 μM) for acute myeloid leukemia research.</p>

<p>iHCK-37 (ASN05260065) is an Hck inhibitor with antitumor activity and blocks HIV-1 replication, used in chronic myelogenous leukemia (CML) research.</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>

<p>Telatinib mesylate is a potent, orally active inhibitor of VEGFR2 (IC50: 6 nM), VEGFR3 (IC50: 4 nM), PDGFα (IC50: 15 nM) and c-Kit (IC50: 1 nM).</p>

<p>BI-4142 is a HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.</p>

<p>IBT6A hydrochloride: Ibrutinib impurity, Btk inhibitor IC50: 0.5 nM, used in dimer/adduct synthesis.</p>

<p>Erlotinib Hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib D6 hydrochloride a deuterium labeled Erlotinib Hydrochloride.</p>

<p>Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5 nM and 303.3 nM for EGFR L858R/T790M and EGFR WT).</p>

<p>(Z)-Orantinib, oral ATP-competitive blocker for Flk-1/KDR, PDGFRβ, FGFR1 (IC50: 2.1, 0.008, 1.2 μM), is a strong antiangiogenic, antitumor drug.</p>

<p>Ponatinib D8 is a deuterium-enriched, oral multi-kinase inhibitor (Abl, PDGFRα, VEGFR2, FGFR1, Src; IC50s: 0.37-5.4 nM).</p>

<p>SU11652 is an effective and competitive receptor tyrosine kinase (RTK) inhibitor, including VEGFR, FGFR, PDGFR, and Kit.</p>

<p>Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.</p>

<p>Iruplinalkib (WX-0593) is an orally active, selective and potent ALK and ROS1 tyrosine kinase inhibitor with anticancer activity for use in the study of non-small cell lung cancer.</p>

<p>(E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent inhibitor of CDK2, JAK2, and FLT3.</p>

<p>Atinvicitinib, a selective JAK1 inhibitor, blocks cytokine signaling, modulating itch, allergy, and inflammatory responses, immune and therapeutic studies.</p>

<p>NX-5948 (BTK-IN-24) is a PROTAC-type BTK degrader with anti-inflammatory and anticancer activities, inhibiting B cell activation.</p>

<p>Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR. Erlotinib D6 is a deuterium labeled Erlotinib .</p>

<p>LDN193189 is a BMPI receptor inhibitor, blocking ALK2 and ALK3 effectively, while weak on ALK4, ALK5, ALK7.</p>

<p>Bleximenib oxalate (Menin-MLL inhibitor 24 oxalate) is a menin-MLL inhibitor that blocks the binding of the menin-KMT2A complex to chromatin at gene promoters.</p>

<p>PGV-1, an oral Curcumin analog, induces apoptosis by inhibiting COX-2, VEGF, and NF-κB activation.</p>

<p>Cediranib maleate (AZD2171 maleate) is a VEGFR2 inhibitor that inhibits Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit.</p>

<p>N-piperidine Ibrutinib hydrochloride is a BTK inhibitor that inhibits WT BTK and C481S BTK , which inhibits the growth and proliferation of cancer cells.</p>

<p>Poseltinib is an oral, irreversible BTK inhibitor (IC50 1.95 nM) with higher selectivity over BMX, TEC, and TXK, blocking BCR, FcR, and TLR signaling.</p>

<p>EW-7195 inhibits ALK5/TGFβR1 (&gt;300x selective over p38α) with 4.83 nM IC50, blocking TGF-β1 signaling, EMT, and breast cancer lung metastasis.</p>

<p>Imatinib D4 is a deuterium-labeled Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, PDGFR, v-Abl, and c-kit kinase activity.</p>

<p>Surfen dihydrochloride (Aminoquinuride dihydrochloride) is a heparin sulfate antagonist with antimicrobial properties and inhibits blockade of signaling.</p>

<p>Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells. Gefitinib D8 is a deuterium labeled Gefitinib.</p>

<p>Ribociclib-d6 is a deuterated compound of Ribociclib (LEE011) for isotope tracing.Ribociclib is an orally available CDK4/6 inhibitor with antitumor activity.</p>

<p>Disitamab (RC48-0) is a humanized anti-HER2 monoclonal antibody used in ADC synthesis.</p>

<p>Aflibercept has a wide range of applications in life science related research.</p>

<p>KG-548 is a dual inhibitor of ARNT/TACC3 and HIF-1α, inhibiting lactate production, and can be used in cancer research.</p>

<p>SM1-71 is a TAK1 inhibitor that inhibits MKNK2 and RSK2.SM1-71 acts as a kinase probe with anticancer activity.</p>

<p>Elsubrutinib (ABBV-105) is a highly active, potent, and selective orally-administered inhibitor of Bruton's tyrosine kinase (BTK). It irreversibly inhibits the catalytic domain of BTK with an IC50 value of 0.18 μM. Elsubrutinib holds potential for the advancement of research on inflammatory diseases.</p>

<p>Itacitinib adipate: oral JAK1 inhibitor, tested in phase II myelofibrosis trial.</p>

<p>Conteltinibtetrahydrochloride (CT-707 tetrahydrochloride) is the tetrahydrochloride form of Conteltinib. It acts as an inhibitor for FAK (IC50=1.6 nM), ALK, and Pyk2. When used in combination with Cabozantinib, Conteltinib tetrahydrochloride exhibits a synergistic antitumor effect.</p>

<p>Afatinib D6 (BIBW 2992 D6) is a deuterium-labeled Afatinib. Afatinib is an irreversible EGFR family inhibitor.</p>

<p>Regorafenib D3 is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor inhibitor of tyrosine kinase.</p>