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tumor targeting agent

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Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-149898

    Transmembrane Glycoprotein Cancer
    Antitumor agent-109 (compound 6) is an inhibitor of hyaluronic acid (HY-B0633A) targeting to CD44, as well as an anti-tumor agent. Hyaluronic acid interacts with differentiation cluster 44 (CD44) and is involved in tumor growth and invasion. Antitumor agent-109 inhibits MDA-MB-231 cells with EC50 value of 0.59 μM .
    HA-CD44 interaction inhibitor 1
  • HY-P0122
    iRGD peptide
    5 Publications Verification

    c(CRGDKGPDC)

    Integrin Cancer
    iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of agents by first binding to αv-integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
    iRGD peptide
  • HY-163545

    Drug Derivative Cancer
    Tc-Me2P is a 99MTC-labeled acrylamide (PnAO) derivative that contains two 4-methyl-2-nitroimidazole groups. The primary activity of Tc-Me2P is as an imaging agent for tumor hypoxia. By specifically binding to hypoxic regions in tumor tissue, it can be used for single photon emission computed tomography (SPECT) and positron emission tomography (PET) imaging to detect hypoxia in tumors. Tc-Me2P can be used to study the targeting of different chemical structures in tumors and normal tissues .
    Tc-Me2P
  • HY-117841

    Microtubule/Tubulin Cancer
    T900607 is an anti-tumor agent and targets microtubule polymerization .
    T900607
  • HY-P10052

    VEGFR Cancer
    CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. CBO-P11 is modified with a nearinfrared cyanine dye bearing an alkyne function, allowing both “click” coupling on azido-modified nanoparticles and fluorescence labelling .
    CBO-P11
  • HY-W520748

    FKBP Cancer
    MJC13 is an FKBP52-targeted agent with anti-tumor activity that can be used in prostate cancer research .
    MJC13
  • HY-128776

    TNF Receptor Cancer
    Antitumor agent-19 is an antitumor agent that targets tumor-associated macrophages (TAMs) and can be used as a potent TAMs modulator. Antitumor agent-19 can increase TNF-alpha levels in tumor cells with EC50 values???of 17.18 μM and 18.87 μM in RAW 264.7 cells and BMDM cells, respectively .
    Antitumor agent-19
  • HY-168953

    P-glycoprotein Apoptosis Bcl-2 Family Reactive Oxygen Species Caspase Cancer
    Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume .
    Lysosomal P-gp targeted agent 1
  • HY-124624

    Microtubule/Tubulin Apoptosis Cancer
    PBOX-15 is a microtubule targeting agent. PBOX-15 induces apoptosis by promoting tubulin depolymerization in tumor cells .
    PBOX-15
  • HY-162348

    Necroptosis Cancer
    Antitumor agent-145 (Compound Ir5) is a tumor inhibitor with remarkable fluorescence and mitochondrial targeting, which exerts anti-cancer effects by inducing necroptosis and activating the necroptosis-related immune response .
    Antitumor agent-145
  • HY-162239

    Others Cancer
    Anticancer agent 187 (Compound 4) is an anticancer agent that can target sarcoma cells in tumor-bearing mouse models. Anticancer agent 187 exhibits cytotoxic activity against HepG2, Caco2, and MCF-7 cells .
    Anticancer agent 187
  • HY-163301

    Reactive Oxygen Species Cancer
    Antitumor agent-139 (compound 9b) is a liver - and mitochondria-targeting gold(I) complexe, and produces reactive oxygen species (ROS) and facilitates DNA excretion. Antitumor agent-139 inhibits tumor growth in a patient-derived xenograft model of hepatocellular carcinoma .
    Antitumor agent-139
  • HY-149019

    c-Kit Apoptosis Cancer
    Antitumor agent-70 (compound 8b) has anti-tumor activity and can induce cell apoptosis. Antitumor agent-70 inhibits multiple myeloma with an IC50 value of 0.12 μM. Antitumor agent-70 is a potential multi-targeted kinase inhibitor especially for c-Kit .
    Antitumor agent-70
  • HY-155034

    Topoisomerase GLUT Cancer
    Antitumor agent-102 (compound 10) is a conjugate of Topoisomerase I inhibitor SN38 and glucose transporter inhibitor, targeting to colorectal cancer. Antitumor agent-102 induces higher concentrations of free SN38 in tumor tissues than Irinotecan (HY-16562) .
    Antitumor agent-102
  • HY-156675A
    Plecstatin-1 hydrochloride
    1 Publications Verification

    Microtubule/Tubulin Cancer
    Plecstatin-1 hydrochloride is an anticancer agent containing organoeuropium. Plecstatin-1 hydrochloride selectively targets plectin, a scaffolding protein and cellular connector, in tumor spheroids .
    Plecstatin-1 hydrochloride
  • HY-159891

    Microtubule/Tubulin Apoptosis Caspase Cancer
    Microtubule destabilizing agent-2 (Compound 21) is an orally active and selective antitumor compound targeting microtubule protein. Microtubule destabilizing agent-2 destabilizes microtubule proteins and inhibits microtubule polymers. Microtubule destabilizing agent-2 arrests the G0/G1 phase in human tumor cells. Microtubule destabilizing agent-2 induces Apoptosis by activating the cascade pathway of caspases. Microtubule destabilizing agent-2 has anti-inflammatory activity, as inhibiting TNF-α and IL-6 in vitro. Microtubule destabilizing agent-2 reduces tumors growth in xenograft mice .
    Microtubule destabilizing agent-2
  • HY-170842

    Apoptosis Cancer
    TDK-HCPT is a small-molecule conjugate that links glutathione-sensitive thiamine disulfide to the chemotherapy drug 10-Hydroxycamptothecin (HY-N0095) via a thioketal bond. TDK-HCPT can target tumor cells and prolong the retention of chemotherapy agents within tumor cells. TDK-HCPT can inhibit tumor growth, induce apoptosis of tumor cells, and has anti-tumor activity .
    TDK-HCPT
  • HY-106168

    NB1011

    Thymidylate Synthase Cancer
    Thymectacin (NB1011) is an agent selectively targeting tumor cells that have a high expression of thymidylate synthase (TS). Thymectacin is an aryloxy phosphoramidate derivative of BVdU (brivudin) .
    Thymectacin
  • HY-W012161

    L-Alanyl-L-phenylalanine; H-Ala-Phe-OH

    Endogenous Metabolite Cancer
    Alanylphenylalanine is a potential antitumor agent that targets DNA via metal coordination. The complex of Alanylphenylalanine and Au (III) can bind to DNA and inhibit tumor cell proliferation[1][2].
    Alanylphenylalanine
  • HY-15855

    Microtubule/Tubulin Cancer
    Fosbretabulin (tromethamine), also known as combretastatin A4 phosphate (CA4P), is a vascular disrupting agent evaluated for its efficacy against anaplastic thyroid carcinoma (ATC). It targets tumor neovasculature, causing acute and reversible reductions in tumor blood flow and central necrosis .
    Fosbretabulin tromethamine
  • HY-16532

    AEZS-108; AN-152

    Peptide-Drug Conjugates (PDCs) GnRH Receptor Cancer
    Zoptarelin doxorubicin (AEZS-108; AN-152) is a hybrid anticancer agent, containing Zoptarelin and Doxorubicin. Zoptarelin doxorubicin has been used to research targeting tumors expressing LHRH receptors. Zoptarelin doxorubicin abolishes tumor progression and induces remarkable apoptosis in vitro .
    Zoptarelin doxorubicin
  • HY-N0093A

    Cyclocytidine; Cyclo-CMP

    DNA/RNA Synthesis CMV Autophagy Cancer
    Ancitabine is the precursor of the anticancer agent Cytarabine (HY-13605), which targets targets related to cell metabolism and proliferation. Ancitabine can inhibit tumor cell proliferation, interfere with the DNA synthesis process of tumor cells, and prevent cell division. Under alkaline pH conditions, Ancitabine can be quantitatively converted into Cytarabine and can be used in the study of cancers such as colorectal cancer .
    Ancitabine
  • HY-N0093
    Ancitabine hydrochloride
    1 Publications Verification

    Cyclocytidine hydrochloride; Cyclo-CMP hydrochloride; Cyclo-C

    Autophagy CMV DNA/RNA Synthesis Cancer
    Ancitabine hydrochloride is the precursor of the anticancer agent Cytarabine (HY-13605), which targets targets related to cell metabolism and proliferation. Ancitabine hydrochloride can inhibit tumor cell proliferation, interfere with the DNA synthesis process of tumor cells, and prevent cell division. Under alkaline pH conditions, Ancitabine hydrochloride can be quantitatively converted into Cytarabine and can be used in the study of cancers such as colorectal cancer .
    Ancitabine hydrochloride
  • HY-151207

    Apoptosis ADC Cytotoxin Cancer
    Anticancer agent 81 (Compound 37b3) is an anticancer agent and can induce tumor cell cycle arrest and apoptosis. Anticancer agent 81 can be used as a payload to conjugate with Trastuzumab (HY-P9907) to obtain the antibody–agent conjugate (ADC) T-PBA. T-PBA maintained its mode of target and internalization ability of Trastuzumab .
    Anticancer agent 81
  • HY-147918

    DNA/RNA Synthesis Cancer
    Anticancer agent 73 (compound CIB-3b) is a anticancer agent, potently targeting TAR RNA-binding protein 2 (TRBP) and disrupts its interaction with Dicer. Anticancer agent 73 can rebalance the expression profile of oncogenic or tumor-suppressive miRNAs. Anticancer agent 73 suppresses the proliferation and metastasis of HCC in vitro and in vivo .
    Anticancer agent 73
  • HY-149718

    JAK HDAC Cancer
    Antitumor agent-123 (Copmound 4d) effectively inhibits multiple kinase targets with anti-cancer effects, including JAK2, JAK3, HDAC1 and HDAC6, with IC50 values of 34.6 and 2.6 μM for JAK2 and JAK3, respectively. Antitumor agent-123 exhibits moderate activity in solid tumor models .
    Antitumor agent-123
  • HY-171331

    PD-1/PD-L1 Integrin Cancer
    AB-3PRGD2 is a radiotherapeutic agent targeting integrin αvβ3. AB-3PRGD2 shows improved tumor uptake and prolonged tumor retention, leading to significantly enhanced tumor growth suppression. AB-3PRGD2 can remodel the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8 + T cells .
    AB-3PRGD2
  • HY-W054292

    (OtBu)KuE(OtBu)2

    PSMA Cancer
    tert-Butyl-DCL is a small molecule PSMAM inhibitor with anticancer activity that targets prostate-specific membrane antigen (PSMA). tert-Butyl-DCL is also an effective bioimaging agent that has high selectivity and affinity, allowing it to target and highlight specific receptors on the surface of tumor cells .
    tert-Butyl-DCL
  • HY-19916A

    BAL-101553 dihydrochloride

    Microtubule/Tubulin Cancer
    Lisavanbulin (BAL-101553) dihydrochloride is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin dihydrochloride exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1 .
    Lisavanbulin dihydrochloride
  • HY-19916

    BAL-101553

    Microtubule/Tubulin Cancer
    Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1 .
    Lisavanbulin
  • HY-146432

    Apoptosis Raf Ras ROS Kinase MDM-2/p53 Cancer
    Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model .
    Antitumor agent-60
  • HY-155485

    Others Cancer
    Abi-DZ-1 is a potential multifunctional theranostic agent via the HIF1α/OATPs Pathway. Abi-DZ-1 can be used in the research of tumor-targeted imaging and precision therapy .
    Abi-DZ-1
  • HY-147699

    Antifolate Cancer
    FRα-IN-1 (Compound 4) is a tumor-targeting agent. FRα-IN-1 shows selective anticancer activity towards folate receptors (FRα and FRβ) expression cells .
    FRα-IN-1
  • HY-13762

    Cytochrome P450 Cancer
    Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
    Tesmilifene
  • HY-13762A

    Cytochrome P450 Cancer
    Tesmilifene hydrochloride is an antihistamine agent and a chemical sensitizer. Tesmilifene hydrochloride targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene hydrochloride overcomes multidrug resistance .
    Tesmilifene hydrochloride
  • HY-P10792

    EGFR Cancer
    HER2-targeted peptide H6F is a HER2 targeting peptide that binds to HER2 to target breast cancer cells, with the amino acid sequence YLFFVFER. The HER2-targeted peptide H6F can be conjugated with the bifunctional chelating agent hydrazinonicotinamide (HYNIC) for radiolabeling with 99mTc. Single-photon emission computed tomography (SPECT) imaging shows that the labeled HER2-targeted peptide H6F specifically accumulates in HER2-positive MDA-MBA-453 tumor-bearing mice models. The HER2-targeted peptide H6F can be used for tumor molecular imaging studies .
    HER2-targeted peptide H6F
  • HY-168717

    Hexokinase Microtubule/Tubulin Reactive Oxygen Species Cancer
    Antitumor agent-190 (Compound 26) is a Hexokinase 2 inhibitor that demonstrates significant anti-tumor activity by targeting microtubules and Hexokinase 2, with an IC50 value of 0.764 μM against MD-MBA-231 cells. Antitumor agent-190 effectively inhibits the activity of Hexokinase 2, leading to the accumulation of Reactive Oxygen Species and dysfunction of the mitochondrial membrane potential (MMP), thereby promoting apoptosis and blocking the cell cycle .
    Antitumor agent-190
  • HY-144793

    Microtubule/Tubulin Cancer
    Deac-SS-Biotin is a potent antitumor agent with improved tumor targeting effects and reduced off-target toxicities. Deac-SS-Biotin uptakes into the cells through biotin-mediated internalization. Deac-SS-Biotin combined with DTT (Glutathione mimetic) can effectively inhibit microtubule assembly and displays greater antitumor activity .
    Deac-SS-Biotin
  • HY-170947

    STAT Quinone Reductase Cancer
    Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
    Antitumor agent-195
  • HY-145406

    Adenosine Receptor HDAC Inflammation/Immunology Cancer
    IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
    IHCH-3064
  • HY-P9968

    EGFR Cancer
    Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a KD of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor agent, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC) .
    Nimotuzumab
  • HY-13622B

    BN 80927 TFA

    Topoisomerase Cancer
    Elomotecan TFA is a potent inhibitor of topoisomerases I and II. Elomotecan TFA is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan TFA reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II .
    Elomotecan TFA
  • HY-13622A

    BN 80927 free base

    Topoisomerase Cancer
    Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II .
    Elomotecan
  • HY-157850

    Microtubule/Tubulin Cancer
    BP-M345 (compound 5) is a potent, cancer cell-targeting antiproliferative agent that exhibits low toxicity to non-tumor cells. BP-M345 inhibits cancer cell proliferation with a GI50 value ranging from 0.17 to 0.45 μM .
    BP-M345
  • HY-13622

    BN 80927

    Topoisomerase Cancer
    Elomotecan hydrochloride (BN 80927) is a potent inhibitor of topoisomerases I and II. Elomotecan hydrochloride (BN 80927) is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan hydrochloride (BN 80927) reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II .
    Elomotecan hydrochloride
  • HY-170779

    FAP Cancer
    DOTA-NI-FAPI-04 is a FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention capabilities. DOTA-NI-FAPI-04 chelates metallic isotopes (such as 68Ga and 177Lu) through DOTA to produce radioactive probes ([ 68Ga]Ga/DOTA-NI-FAPI-04 and [ 177Lu]Lu/DOTA-NI-FAPI-04), which can be used for research in tumor diagnostics and therapeutic agents. DOTA-NI-FAPI-04 holds dual targeting potential in the fields of cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly suitable for scenarios where the tumor stroma and hypoxic regions synergistically interact .
    DOTA-NI-FAPI-04
  • HY-13762S

    Isotope-Labeled Compounds Cytochrome P450 Cancer
    Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
    Tesmilifene-d4
  • HY-P99233

    HuMax-TAC

    Interleukin Related Cancer
    Camidanlumab (HuMax-TAC) is a CD25 monoclonal antibody. Camidanlumab targets the cell-surface antigen CD25, which is over-expressed on a variety of hematological tumors and shows limited expression on normal tissues. Camidanlumab can be used for synthesis of antibody agent conjugates (ADCs) to research several diseases including lymphoma and leukemia .
    Camidanlumab
  • HY-173211

    Photosensitizer Cancer
    anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic agent targeting mitochondrial DNA G4 (mtG4). Under white light irradiation, its IC50 against 4T1 cells is 0.42 μM. anti-TNBC agent-8 binds tightly to mtG4 and generates a large amount of reactive oxygen species (ROS) under white light irradiation, leading to the loss of mitochondrial membrane potential (MMP), a decrease in ATP production, and an increase in the ROS level. This, in turn, induces significant apoptosis in triple-negative breast cancer (TNBC) cells, exerting the activity of inhibiting tumor cell growth. anti-TNBC agent-8 can be used in the research of triple-negative breast cancer.
    anti-TNBC agent-8
  • HY-16350

    NKP-1339; IT-139; KP-1339

    DNA/RNA Synthesis Apoptosis Cancer
    BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu .
    BOLD-100

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