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Tumor selectivity

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934

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2

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5

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8

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40

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20

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-163548

    Sialyltransferase Cancer
    SPP-002 is a sulfate analogue that acts as a potential Sialyltransferase (ST) inhibitor. SPP-002 selectively inhibits n-glycosialylation with inhibition at least an order of magnitude greater than that of unmodified parental cholic acid (LCA). SPP-002 reduces tumor cell migration and invasion by inhibiting the integrin /FAK/Paxillin signaling pathway. SPP-002 can be used in the study of tumor metastasis .
    SPP-002
  • HY-138742

    MAP4K Cancer
    HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 .
    HPK1-IN-7
  • HY-110201

    Estrogen Receptor/ERR Cancer
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
    Estrogen receptor modulator 1
  • 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-16405

    DNA Alkylator/Crosslinker Cancer
    PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
    PR-104
  • HY-143889

    CDK Cancer
    Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
    Senexin C
  • HY-147784

    Btk Cancer
    HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models .
    HZ-A-005
  • HY-123130

    MMP Cancer
    ABT-770 (compound 11) is a highly selective and orally active MMP inhibitor, demonstrating over 1000-fold selectivity for MMP-2 (IC50=4 nM) compared to MMP-1 (IC50=4600 nM). ABT-770 can be utilized in studies related to tumor growth, invasion, and metastasis .
    ABT-770
  • HY-16406

    DNA Alkylator/Crosslinker Cancer
    PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
    PR-104 sodium
  • HY-143439

    Estrogen Receptor/ERR Cancer
    LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity .
    LX-039
  • HY-18969

    CDK Cancer
    LDC3140 is a selective CDK7 inhibitor (IC50<5 nM). By inhibiting the activity of CDK7, LDC3140 affects the regulation of the cell cycle, leading to cell cycle arrest and thus inhibiting the proliferation of tumor cells. LDC3140 can be used in the research of cancer treatment .
    LDC3140
  • HY-P10388

    CD47 TGF-β Receptor Cancer
    TAX2 peptide is a dodecapeptide based on molecular docking and simulation design, derived from the cell surface receptor CD47 sequence. TAX2 peptide acts as a selective antagonist of TSP-1 (thromboxin-1) interacting with CD47. TAX2 peptide can promote the binding of TSP-1 to CD36, which leads to the destruction of VEGFR2 (vascular endothelial growth factor receptor 2) activation, thereby blocking downstream NO (nitric oxide) signaling, demonstrating anti-angiogenic properties. TAX2 peptide can be used to study angiogenesis and tumor cell interactions in the tumor microenvironment .
    TAX2 peptide
  • HY-175809

    CD44 Src EGFR MAPKAPK2 (MK2) Cancer
    SRT6, an anticancer agent is a CD44 inhibitor. SRT6 inhibits key CD44-associated kinases, including SRC, ERBB2 and MAPKAPK2. SRT6 has strong tumor selectivity over non-tumoral lung cells and significant antiproliferative activity against cancer cells (EC50of 1.37  μM for NCI-H23 cells) .
    SRT6
  • HY-130612

    Epigenetic Reader Domain PROTACs Cancer
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
    PROTAC BRD2/BRD4 degrader-1
  • HY-172930

    Molecular Glues IKZF Family Potassium Channel Inflammation/Immunology Cancer
    PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50  of  0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn 391V C57BL/6 mice .
    PVTX-405
  • HY-163146

    Fluorescent Dye Cancer
    TME-HYM (PH Probe) is a novel fluorescent probe based on acidic tumor microenvironment (TME) activation and organic anion transporting polypeptide (OATPs, overexpressed on cancer cells), and can be selective uptaken. TME-HYM (PH Probe) can selectively lit up cancer cells and tumor tissues, offering dual tumor selectivity for precise visualization of tumor mass .
    TME-HYM (PH Probe)
  • HY-117412

    Drug Derivative Cancer
    KCG 1 is a potent and selective anti-tumor agent that displays anti-prollferative and cytotoxic effects on epithelial tumoral cells .
    KCG 1
  • HY-136979
    RBN012759
    5+ Cited Publications

    PARP Inflammation/Immunology Cancer
    RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants .
    RBN012759
  • HY-P1007

    Z-VE(OMe)ID(OMe)-FMK

    Caspase Apoptosis Cancer
    Z-VEID-FMK (Z-VE(OMe)ID(OMe)-FMK) is a selective and irreversible caspase-6 peptide inhibitor. Z-VEID-FMK alleviates the drug-induced augmentation of caspase-6 activity, DNA fragmentation, and cell apoptosis .
    Z-VEID-FMK
  • HY-175023

    Others Cancer
    OncoACP3 (Compound s43) is a high affinity ligand for prostatic acid phosphatase (ACP3). OncoACP3, radiolabelled with Lu-177, selectively accumulates in enzyme-expressing tumors and shows a potent anti-tumor activity with excellent tumor-selective payload deposition in HT1080.hACP3 and PC3.hACP3 tumor-bearing mice model. OncoACP3 can be used for prostate cancer research .
    OncoACP3
  • HY-P2526
    LyP-1
    2 Publications Verification

    Complement System Cancer
    LyP-1 is a cyclic 9-amino-acids tumor homing peptide and selectively bind to p32 receptors overexpressed in various tumor-associated cells .
    LyP-1
  • HY-175023A

    Others Cancer
    OncoACP3 TFA (Compound s43) is a high affinity ligand for prostatic acid phosphatase (ACP3). OncoACP3 TFA, radiolabelled with Lu-177, selectively accumulates in enzyme-expressing tumors and shows a potent anti-tumor activity with excellent tumor-selective payload deposition in HT1080.hACP3 and PC3.hACP3 tumor-bearing mice model. OncoACP3 TFA can be used for prostate cancer research .
    OncoACP3 TFA
  • HY-121087
    BCI-215
    3 Publications Verification

    Phosphatase Cancer
    BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells .
    BCI-215
  • HY-128587
    Mevociclib
    4 Publications Verification

    SY-1365

    CDK Cancer
    Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors .
    Mevociclib
  • HY-112243

    CDK Inflammation/Immunology Cancer
    Cimpuciclib is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity .
    Cimpuciclib
  • HY-112243A

    CDK Inflammation/Immunology Cancer
    Cimpuciclib tosylate is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity .
    Cimpuciclib tosylate
  • HY-50895A
    Gefitinib hydrochloride
    170+ Cited Publications

    ZD-1839 hydrochloride

    EGFR Cancer
    Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity .
    Gefitinib hydrochloride
  • HY-101566A
    Elimusertib hydrochloride
    10+ Cited Publications

    BAY 1895344 hydrochloride

    ATM/ATR Cancer
    Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity . Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas .
    Elimusertib hydrochloride
  • HY-13646C

    HM30181 mesylate hydrochloride; HM30181A mesylate hydrochloride

    P-glycoprotein Cancer
    Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models .
    Encequidar mesylate hydrochloride
  • HY-P99547

    (vic)-Trastuzumab duocarmazine

    Antibody-Drug Conjugates (ADCs) Cancer
    Trastuzumab duocarmazine ((vic)-Trastuzumab duocarmazine) is a HER2-targeting ADC that is recognized and cleaved by histone B in tumor cells and selectively targets tumor cells. Trastuzumab duocarmazine has anti-tumor activity and can be used in cancer research related to uterine and ovarian sarcomas .
    Trastuzumab duocarmazine
  • HY-P9978

    PD-1/PD-L1 Cancer
    Toripalimab is a selective, recombinant, humanized monoclonal antibody against PD-1. Toripalimab is able to bind to PD-1 and block the interaction with its ligands. Toripalimab has exhibited primary anti-tumor effects in tumors such as melanoma, lung cancer, digestive tract tumors, hepatobiliary and pancreatic tumors, neuroendocrine neoplasms, nasopharyngeal carcinoma and urothelial carcinoma .
    Toripalimab
  • HY-101566
    Elimusertib
    10+ Cited Publications

    BAY 1895344

    ATM/ATR Cancer
    Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity . Elimusertib can be used for the research of solid tumors and lymphomas .
    Elimusertib
  • HY-164827

    CDK Cancer
    CDK2 degrader 3 can selectively degrade CDK2 and has anti-tumor activity .
    CDK2 degrader 3
  • HY-143510

    mTOR Cancer
    RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth.
    RMC-4627
  • HY-153268

    BDTX-1535; EGFR-IN-76

    EGFR Cancer
    BDTX-1535 (EGFR-IN-76) is an orally available, blood-brain permeable, selective EGFR inhibitor with anti-tumor activity. BDTX-1535 is indicated in a variety of models including non-small cell lung cancer, glioblastoma patient-derived tumors, and intracranial tumors .
    Silevertinib
  • HY-137813

    PERK Neurological Disease Metabolic Disease Cancer
    PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states .
    PERK-IN-4
  • HY-150266

    Bcl-2 Family Cancer
    A-1293102 is a potent and selective BCL-XL inhibitor that kills BCL-XL-dependent tumor cells .
    A-1293102
  • HY-133779

    Drug Metabolite Others Cancer
    Gefitinib impurity 5 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
    Gefitinib impurity 5
  • HY-131257

    Drug Metabolite Others Cancer
    Gefitinib impurity 1 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
    Gefitinib impurity 1
  • HY-151425

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    TDO-IN-1 is an orally active and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), shows excellent selectivity over indoleamine-2,3-dioxygenase (IDO), with an IC50 value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo .
    TDO-IN-1
  • HY-124711
    TBOPP
    1 Publications Verification

    DOCK Cancer
    TBOPP is a selective inhibitor of DOCK1 with an IC50 of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with high affinity (Kd of 7.1 μM), has anti-tumor activity for broader types of tumors .
    TBOPP
  • HY-12710

    α-Yohimbine; Corynanthidine; Isoyohimbine

    Adrenergic Receptor Cancer
    Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis .
    Rauwolscine
  • HY-50895S1

    ZD1839-d6

    EGFR Autophagy Cancer
    Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
    Gefitinib-d6
  • HY-153358

    HDAC Cancer
    TNG260 is a selective, orally effective inhibitor of HDAC1 and CoREST complex, with a 10-fold selectivity for HDAC1 over HDAC3 and a 500-fold selectivity for CoREST complex over NuRD and Sin3 complex. TNG260 reshapes the tumor immune microenvironment, reduces immunosuppressive neutrophil infiltration, promotes effector T cell recruitment, and reverses anti-PD-1 resistance caused by STK11 deficiency by inhibiting the activity of the CoREST-HDAC1 complex. TNG260 induces durable tumor regression in combination with α-PD1 in MC38 tumor-bearing mice with STK11 mutations, and has lower toxicity to bone marrow cells than non-selective HDAC inhibitors .
    TNG260
  • HY-149616

    PROTACs ERK Cancer
    PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC50 of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages .
    PPM-3
  • HY-175361

    ROR Cancer
    RORγ agonist 2 (Compound 34) is a selective RORγ agonist with an EC50 of 0.03  μM for hRORγ. RORγ agonist 2 significantly inhibits tumors growth in syngeneic MC38 tumor mice model .
    RORγ agonist 2
  • HY-168280

    Ligands for E3 Ligase Cancer
    AS1411-C4-VH032 (AS1411-VH032) promotes tumor-selective degradation of MDM2, leading to tumor shrinkage without detectable toxicity .
    AS1411-C4-VH032
  • HY-111213

    Histone Methyltransferase Cancer
    PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity .
    PRMT5-IN-20
  • HY-112181
    KO-947
    4 Publications Verification

    ERK Cancer
    KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.
    KO-947
  • HY-151590

    HDAC Cancer
    DKFZ-748 is a selective HDAC10 inhibitor (pIC50=7.66), and shows anti-tumor activity .
    DKFZ-748

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