Angiogénese

<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>Sotiburafusp alfa is a humanized bispecific fusion protein comprising a VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) connected</p>

<p>JAK/HDAC-IN-2, a potent 2-amino-4-phenylaminopyrimidine dual-target inhibitor, effectively suppresses JAK1/2 and HDAC3/6 at nanomolar concentrations.</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>Phage display selected Affibody ligands for HER2/neu from a protein library based on a 58-residue Staphylococcal protein A Z domain.</p>

<p>EGFR-IN-42 (17b) is a potent EGFR inhibitor with nanomolar efficacy, merging tamoxifen/endoxifen and gefitinib, exhibiting enhanced anti-cancer action.</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>Potent, selective oral PROTAC BTK Degrader-1; IC50: 34.51 nM (WT), 64.56 nM (BTK-481S); reduces BTK protein, inhibits tumors.</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>ML228 activates HIF pathway and VEGF, with EC50 of 1μM, effective in vitro.</p>

<p>EGFRT790M/L858R-IN-2: selective inhibitor, IC50: 3.5 nM (mutant), 1290 nM (WT); reduces p-EGFR/AKT/ERK1/2, triggers apoptosis, G1 arrest, anti-cancer.</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>(R)-3-Hydroxy Midostaurin: potent kinase inhibitor, major midostaurin metabolite via CYP3A4, potential AML treatment.</p>

<p>AZ7550 trimesylate salt (AZ7550 Mesylate) is the active metabolite of ositinib, AZ7550 inhibits IGF1R activity and can be used in the study of lung cancer.</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>ALK/ROS1-IN-5 (compound X4) is a selective inhibitor of ALK and ROS1 kinases, with IC50 values of 0.512 μM for ALK and 0.766 μM for ROS1. It inhibits H2228 cells with an IC50 of 0.034 μM and induces apoptosis in cancer cells in a dose-dependent manner. Additionally, ALK/ROS1-IN-5 effectively suppresses the expression of p-ALK and p-ERK in cancer cells.</p>

<p>EGFR-IN-22: potent for EGFR (IC50: 4.91 nM) &amp; L858R/T790M/C797S mutation (IC50: 0.54 nM).</p>

<p>VSLRGDTRG acetate is a synthetic peptide of the RGD motif from cadherin17 (CDH17), capable of binding to α2β1 integrin and activating its signaling pathways. It facilitates the high-affinity conformational change of β1 integrin via the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby promoting tumor proliferation and metastasis. VSLRGDTRG acetate is applicable in research on cancers expressing CDH17, such as colon and pancreatic cancers.</p>

<p>A unique collection of 1353 proangiogenic and antiangiogenic compounds for new targets identification, research in mechanisms of angiogenesis, and high</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>DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP[1].</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>SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker.</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>AMT-562 is an antibody-drug conjugate (ADC) composed of a novel anti-HER3 antibody, Ab562, linked to the linker Mc-VC-PAB and the topoisomerase I inhibitor, Exatecan. The ADC's toxic component and linker are represented as MC-VA-PAB-Exatecan. AMT-562 can induce apoptosis and exhibits antitumor activity against pancreatic, esophageal, and gastric cancers.</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>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>NRX-0492: orally active BTK degrader, induces ubiquitylation/proteasomal breakdown, potent with DC50 ≤0.2 nM, DC90 ≤0.5 nM, disrupts BCR signaling.</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>

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>EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting the mutations EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S. This compound shows potential in addressing acquired resistance in the treatment of non-small cell lung cancer.</p>

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

<p>EGFR-IN-110 (Compound 6) is a covalent inhibitor of EGFR, demonstrating pIC50 values of 9.2 for the EGFR enzyme and 8.7 for EGFR cells. It exhibits strong efficacy in targeting EGFR and maintains good kinase selectivity.</p>

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

<p>FW-1 is a type I inhibitor of FLT3, with an IC50 of approximately 1 μM. It exhibits cytotoxic effects in FLT3-mutant AML cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis in MV4-11 and MOLM-13 cells.</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>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>Tirbanibulin is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).</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>iHCK-37 (ASN05260065) is an Hck inhibitor with antitumor activity and blocks HIV-1 replication, used in chronic myelogenous leukemia (CML) research.</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>Tetrac (Tetraiodothyroacetic acid) is a derivative of L-thyroxine (T4), a thyroxine integrin receptor antagonist.Tetrac induces antiproliferation by blocking</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>BI-4142 is a HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.</p>

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

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

Pazopanib-d6 is a deuterated compound of Pazopanib.

SB1317 (TG02) is a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3).

<p>Ponatinib D8 is a deuterium-enriched, oral multi-kinase inhibitor (Abl, PDGFRα, VEGFR2, FGFR1, Src; IC50s: 0.37-5.4 nM).</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>Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.</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>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>NX-5948 (BTK-IN-24) is a PROTAC-type BTK degrader with anti-inflammatory and anticancer activities, inhibiting B cell activation.</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>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>Cediranib maleate (AZD2171 maleate) is a VEGFR2 inhibitor that inhibits Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit.</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>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>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>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>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>Aflibercept has a wide range of applications in life science related research.</p>

<p>Disitamab (RC48-0) is a humanized anti-HER2 monoclonal antibody used in ADC synthesis.</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>KG-548 is a dual inhibitor of ARNT/TACC3 and HIF-1α, inhibiting lactate production, and can be used in cancer research.</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>