Angiogénesis

<p>M4205 is an inhibitor of c-Kit exhibiting high activity on c-Kit mutations in exons 11, 13, 17.</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>Necitumumab (IMC-11F8) is a human monoclonal antibody against EGFR, an anti-angiogenic agent used in the treatment of advanced non-small cell lung cancer.</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>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>EP26 is an orally active and potent inhibitor of EGFR and PD-L1, with IC50 values of 48.6 nM and 1.77 µM, respectively. It reduces the protein expression of p-EGFR and induces cell cycle arrest at the G0/G1 phase. EP26 shows potential for glioblastoma research.</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>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>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>PROTAC ALK degrader-3 (4B) is an orally active PROTAC-based ALK degrader, efficiently inducing sustained degradation of ALK fusion protein and significant inhibition of downstream pathways in Karpas 299 cells with an IC50 of 119.33 nM. This compound exhibits antitumor activity.</p>

<p>AT-533 inhibits Hsp90, HSV, hinders HIF-1α/VEGF/VEGFR-2, Erk1/2, FAK, Akt/mTOR/p70S6K, and blocks tumor growth, angiogenesis, and HUVEC activities.</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>BRK inhibitor P21d HCl targets breast tumor kinase with 30 nM IC50, suppresses p-SAM68 at 52 nM, useful for in vivo breast cancer research.</p>

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

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

<p>EGFR-IN-93 (compound 18) is an allosteric inhibitor of the T790M/L858R double mutant EGFR. It is applicable for research in non-small cell lung cancer (NSCLC).</p>

<p>Lewis Y tetrasaccharide, a derivative of Lewis X, is an antigen linked to ovarian cancer metastasis and bad prognosis.</p>

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

<p>EGFR-IN-95 is a derivative of 2,4-diaminonicotinamide. It effectively inhibits the activity of EGFRdel19/T790M/C797S and L858R/T790M/C797S.</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>PROTACBTK Degrader-8 (compound 3) is an efficient PROTAC BTK degrader with a linker that can couple with ADC antibodies to form PAC.</p>

<p>EGFRWT/T790M/L858R-IN-1 (compound 10d) is a potent inhibitor of EGFR, demonstrating IC50 values of 0.097, 0.280, and 0.051 μM for EGFRWT, EGFRT790M, and EGFRL858R, respectively. This compound can be utilized in cancer research.</p>

PROTAC VEGFR-2 degrader-1 shows minimal VEGFR-2 inhibition & low anti-proliferative effect on EA.hy926 cells.

<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>GMB-475 is a PROTAC ligand targeting BCR-ABL1 for degradation via E3 ligase recruitment.</p>

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

<p>Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9) is a peptide derived from mouse JAK2, specifically composed of amino acids 475 to 491.</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>

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

<p>HER2-IN-20 (compound 32) is a potent and selective inhibitor of HER2WT and HER2YVMA, with IC50 values of 49 and 42 nM, respectively. It holds potential for research in non-small cell lung cancer (NSCLC).</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>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>PEPvIII, a peptide sequence from EGFRvIII, was designed to represent a target of glioma and is presented by MHC I/II complexes.</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>PROTAC TYK2 Agent1 selectively degrades TYK2, with a 14 nM DC50, for autoimmune research.</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>DB1113 is a bifunctional kinase degrader, targeting ABL1, ABL2, CDK4, MAPKs, and more for disease research.</p>

<p>SIAIS100, a potent BCR-ABL PROTAC degrader, demonstrates a DC50 value of 2.7 nM, highlighting its efficacy.</p>

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

<p>Tovecimig is a G1-scFvlh_L-κ type bispecific antibody targeting VEGFA/DLL4.</p>

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

<p>U3-1565 (Anti-HB-EGF antibody) is an antibody targeting HB-EGF with potential anti-tumor activity, used in the study of advanced solid tumors.</p>

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

<p>VGX100 is a humanized antibody targeting VEGFC for the study of solid 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>KG-548 is a dual inhibitor of ARNT/TACC3 and HIF-1α, inhibiting lactate production, and can be used in cancer research.</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>Regorafenib D3 is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor inhibitor of tyrosine kinase.</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>Erlotinib Hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib D6 hydrochloride a deuterium labeled Erlotinib Hydrochloride.</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>Lck inhibitor 2 blocks tyrosine kinases LCK, BTK, LYN, SYK, TXK with IC50s: Lck 13nM, Btk 9nM/26nM, Lyn 3nM, Txk 2nM.</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>(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>LDN193189 is a BMPI receptor inhibitor, blocking ALK2 and ALK3 effectively, while weak on ALK4, ALK5, ALK7.</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>Cediranib maleate (AZD2171 maleate) is a VEGFR2 inhibitor that inhibits Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit.</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>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>Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.</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>QL47 acts as an inhibitor of viral translation and a BTK inhibitor with antiviral activity against dengue virus and can be used in the study of lymphoma.</p>

<p>Ifidancitinib (ATI-50002) is a JAK kinase 1/3 inhibitor used to study autoimmune diseases.</p>

<p>Tyrphostin 8(4-Hydroxybenzylidenemalononitrile) is a potent GTPase inhibitor that inhibits EGFR kinase with an IC50 of 560 μM.Tyrphostin 8 inhibits protein</p>

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

<p>HIF-IN-1 is a inhibitor of hypoxia-inducible factor, which is associated with tumor and cancer cell proliferation and inhibits HIF-1α protein aggregation.</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>iHCK-37 (ASN05260065) is an Hck inhibitor with antitumor activity and blocks HIV-1 replication, used in chronic myelogenous leukemia (CML) 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>FLT3-IN-16 is a potent FLT3 inhibitor (IC50 = 1.1 μM) for acute myeloid leukemia 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>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>(3S, 4S)-PF-06459988, a less active S enantiomer, specifically inhibits T790M mutant EGFR with high selectivity.</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>(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>Tirbanibulin is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).</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>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>

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

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

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