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primary tumor

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33

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2

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153450
    JBI-589

    		Protein Arginine Deiminase Cancer
    JBI-589 is a non-covalent PAD4 isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research .
    JBI-589
  • HY-153863
    MS934

    		PROTACs MEK Cancer
    MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 has anti-proliferation potency at inhibiting the growth of HT-29 cells with a GI50 value of 0.023 μM. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma .
    (Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078))
    MS934
  • HY-P9978
    Toripalimab

    		PD-1/PD-L1 Cancer
    Toripalimab is the first domestic anti-tumor PD-1 antibody in China. 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-107999
    CADD522
    3 Publications Verification

    		 Reactive Oxygen Species Cancer
    CADD522 is a RUNX2-DNA binding inhibitor (downregulates RUNX2-mediated transcription of downstream target genes), with an IC50 of 10 nM. CADD522 inhibits primary tumor growth and experimental metastasis of tumor cells in the lungs of immune-compromised mice. CADD522 can be used in study of cancer .
    CADD522
  • HY-A0037
    Lasofoxifene
    4 Publications Verification

    CP-336156

    		 Estrogen Receptor/ERR Inflammation/Immunology Cancer
    Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis .
    Lasofoxifene
  • HY-147250A
    Lirafugratinib hydrochloride

    RLY-4008 hydrochloride

    		 FGFR Cancer
    Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
    Lirafugratinib hydrochloride
  • HY-126730
    Rubratoxin A

    		Phosphatase Cancer
    Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts .
    Rubratoxin A
  • HY-16477A
    Talaporfin

    ME2906 free acid; Mono-L-aspartyl chlorin e6 free acid; NPe6 free acid

    		 Others Cancer
    Talaporfin sodium, can be used in intraoperative photodynamic therapy (PDT) with a 664-nm semiconductor laser, was evaluated for efficacy and safety in treating primary malignant parenchymal brain tumors .
    Talaporfin
  • HY-103407
    PD 168568

    		Dopamine Receptor Neurological Disease Cancer
    PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research .
    PD 168568
  • HY-124875
    Arylsulfonamide 64B

    HIF inhibitor 64B

    		 HIF/HIF Prolyl-Hydroxylase Neurological Disease
    Arylsulfonamide 64B (HIF inhibitor 64B) is an inhibitor of the hypoxia-induced factor (HIF). Arylsulfonamide 64B inhibits hypoxia/HIF-induced expression of c-Met and CXCR4 and reduces primary tumor growth and metastasis of uveal melanoma mouse model .
    Arylsulfonamide 64B
  • HY-147250
    Lirafugratinib

    RLY-4008

    		 FGFR Cancer
    Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
    Lirafugratinib
  • HY-119618
    R1498

    		Endogenous Metabolite Cancer
    R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
    R1498
  • HY-A0038
    Lasofoxifene tartrate
    4 Publications Verification

    CP-336156 tartrate

    		 Estrogen Receptor/ERR Endocrinology Cancer
    Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM) . Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis .
    Lasofoxifene tartrate
  • HY-163545
    Tc-Me2P

    		Others 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-P9983
    Lintuzumab

    HuM-195

    		 Others Radionuclide-Drug Conjugates (RDCs) Inflammation/Immunology
    Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR? and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .
    Lintuzumab
  • HY-144670
    ALDH3A1-IN-1

    		Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH3A1-IN-1 (Compound 18) is a potent inhibitor of ALDH3A1 with an IC50 of 1.61 μM. ALDH3A1-IN-1 is more potent than DEAB against patient-derived primary prostate tumor epithelial cells, as single agents or in combination research with docetaxel .
    ALDH3A1-IN-1
  • HY-19471
    (rac)-ZK-304709

    		Others Cancer
    (rac)-ZK-304709 is an isomer of ZK-304709. It is a first-in-class oral multi-target tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (Cdks), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. It directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. In an orthotopic BON tumor model, (rac)-ZK-304709 reduced primary tumor growth by 80% and reduced tumor microvascular density. These results suggest that (rac)-ZK-304709 can effectively control tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may be a potential agent for the treatment of NET.
    (rac)-ZK-304709
  • HY-40136S
    cis-4-Hydroxy-L-proline-d3

    		Isotope-Labeled Compounds Endogenous Metabolite Cancer
    cis-4-Hydroxy-L-proline-d3 is the deuterium labeled cis-4-Hydroxy-L-proline. cis-4-Hydroxy-L-proline, a proline analogue, is an inhibitor of collagen production. cis-4-Hydroxy-L-proline could inhibit fibroblast growth by preventing the deposition of triple-helical collagen on the cell layer. cis-4-Hydroxy-L-proline also depresses the growth of primary N-nitrosomethylurea-induced rat mammary tumors[1][2][3][4].
    cis-4-Hydroxy-L-proline-d3
  • HY-133016
    M8891

    		MetAP Cardiovascular Disease Cancer
    M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM) . M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity .
    M8891
  • HY-105017
    Evodenoson

    ATL 313; DE 112

    		 Adenosine Receptor Infection Inflammation/Immunology
    Evodenoson is a selective agonist of the A2A adenosine receptor. Evodenoson’s primary actions include reducing inflammatory responses, decreasing intestinal fluid secretion, edema, tissue damage, and neutrophil infiltration induced by Clostridium difficile toxin A. Evodenoson’s protective effect is achieved by reducing myeloperoxidase (MPO) and adenosine deaminase (ADA) activities, and by lowering the production of tumor necrosis factor-alpha (TNF-α) .
    Evodenoson
  • HY-40136
    cis-4-Hydroxy-L-proline

    		Endogenous Metabolite Metabolic Disease Cancer
    cis-4-Hydroxy-L-proline, a proline analogue, is an inhibitor of collagen production. cis-4-Hydroxy-L-proline could inhibit fibroblast growth by preventing the deposition of triple-helical collagen on the cell layer. cis-4-Hydroxy-L-proline also depresses the growth of primary N-nitrosomethylurea-induced rat mammary tumors .
    cis-4-Hydroxy-L-proline
  • HY-W338764
    AHR agonist 3

    		Apoptosis Aryl Hydrocarbon Receptor Cancer
    AHR agonist 3 is an aryl hydrocarbon receptor (AhR) agonist, that can induces cell cycle arrest or apoptosis via activation of tumor-suppressive transcriptional programs. AHR agonist 3 inhibits triple-negative breast cancer (TNBC) stem cell growth via AhR while exhibits minimal cytotoxicity against normal human primary cells and can be used for cancer research .
    AHR agonist 3
  • HY-149913
    NR2F1 agonist 1

    		Others Cancer
    NR2F1 agonist 1, a nuclear receptor NR2F1 agonist, specifically activates dormancy programs in malignant cells. NR2F1 agonist 1 up-regulates NR2F1 and downstream target genes that regulate dormancy. NR2F1 agonist 1 induces neural crest-like and growth suppression in head and neck squamous cell carcinoma (HNSCC) via NR2F1 activation. NR2F1 agonist 1 inhibits tumor growth in a mouse primary tumor model .
    NR2F1 agonist 1
  • HY-110243
    CAIX Inhibitor S4
    1 Publications Verification

    		 Carbonic Anhydrase Cancer
    CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth .
    CAIX Inhibitor S4
  • HY-108417
    Debio 0617B

    		STAT JAK Bcr-Abl Cancer
    Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34 + stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors .
    Debio 0617B
  • HY-155446
    di-DTPA-LTL

    		Others Inflammation/Immunology Cancer
    di-DTPA-LTL is a bivalent hapten based on tyrosine-containing polypeptide design. di-DTPA-LTL has good hydrophilia and biological distribution. di-DTPA-LTL is labeled with 111In (indium) and 131I (iodine). di-DTPA-LTL achieves tumor radioimmunoimaging in primary colorectal cancer patients with CEA by injecting a fixed low dose (5 mg) of bispecific antibody (anti-CEA x, anti-DTPA) and di-DTPA antigen peptide (labeled 111In) into the patients .
    di-DTPA-LTL
  • HY-164689
    Cadmium pyrithione

    		Others Cancer
    Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models .
    Cadmium pyrithione
  • HY-146260
    NVP-CLR457

    		PI3K Cancer
    NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity .
    NVP-CLR457
  • HY-40136R
    cis-4-Hydroxy-L-proline (Standard)

    		Endogenous Metabolite Metabolic Disease Cancer
    cis-4-Hydroxy-L-proline (Standard) is the analytical standard of cis-4-Hydroxy-L-proline. This product is intended for research and analytical applications. cis-4-Hydroxy-L-proline, a proline analogue, is an inhibitor of collagen production. cis-4-Hydroxy-L-proline could inhibit fibroblast growth by preventing the deposition of triple-helical collagen on the cell layer. cis-4-Hydroxy-L-proline also depresses the growth of primary N-nitrosomethylurea-induced rat mammary tumors [4].
    cis-4-Hydroxy-L-proline (Standard)
  • HY-149295
    PROTAC ERα Degrader-4

    		PROTACs Estrogen Receptor/ERR Apoptosis Cancer
    PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER + breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
    PROTAC ERα Degrader-4
  • HY-162874
    diABZI-V/C-DBCO

    		STING Inflammation/Immunology Cancer
    diABZI-V/C-DBCO (Compound 3) is a potent STING agonist. diABZI-V/C-DBCO can release diABZI-amine upon activation by cathepsin B to activate STING, leading to the production of interferons and other immune-stimulatory molecules, thereby enhancing the immune system's response to tumors. The EC50 values for diABZI-V/C-DBCO and diABZI-amine in activating STING in THP1-Dual cells are 1.47 and 0.144 nM, respectively, and in primary mouse splenocytes, the EC50 values are 7.7 and 0.17 μM, respectively. diABZI-V/C-DBCO can be used in cancer immunotherapy research .
    diABZI-V/C-DBCO
  • HY-117051
    STA-2842

    		Others Cancer
    STA-2842 is a small molecule agent that inhibits heat shock protein 90 (HSP90) to treat autosomal dominant polycystic kidney disease (ADPKD). The disease is caused by inherited mutations in the PKD1 or PKD2 genes that aberrantly activate multiple signaling proteins and pathways that regulate cell proliferation. Through network construction, we found that many HSP90 client proteins associated with ADPKD are regulated by HSP90. STA-2842 induced degradation of these clients in Pkd1?/? primary kidney cells and in vivo. In experiments using conditional Cre-mediated in vivo knockout of Pkd1 in mice, we found that weekly administration of STA-2842 for 10 weeks significantly reduced initial renal cyst formation and kidney growth in mice and slowed disease progression in mice with pre-existing cysts. These improved disease phenotypes were accompanied by improvements in renal function markers and reductions in the expression and activity of HSP90 clients and their effectors, with the extent of this inhibition correlating with the extent of cyst expansion in individual animals. Pharmacokinetic analysis showed that HSP90 was overexpressed in cystic kidney tissue and HSP90 inhibitors were selectively retained in cystic tissue, which is similar to the situation in solid tumors. These results provide a preliminary basis for evaluating HSP90 inhibitors as therapeutic agents for ADPKD.
    STA-2842
  • HY-117019
    LY150310 free base

    		Others Cancer
    LY150310 is able to inhibit thromboxane synthase, cyclooxygenase, and thrombin activation, biochemical processes that have been proposed in the literature as targets for anti-metastatic agents. The objectives of this study were twofold: (a) to compare the anti-metastatic activity of Eli Lilly compounds with reference anti-metastatic compounds nafazatrom and RA233; and (b) to examine the correlation between inhibition of spontaneous lung metastasis and survival. The anti-metastatic activity of the compounds was evaluated using the Lewis lung squamous cell carcinoma cell model. In this model, 5×10^5 tumor cells were implanted into the gastrocnemius muscle, the primary tumor was resected on day 14, and lung metastatic lesions were counted on day 25. The compounds were administered every 12 hours from day 5 to day 19. Nafazatrom, LY150310, LY189332, and LY135305 were found to inhibit spontaneous lung metastasis in a dose-dependent manner. The ED50 values ??of these compounds were 50, 0.5, 2, and 0.35 mg/kg/day, respectively; the corresponding therapeutic indices (LD50/ED50) were 7, 180, 255, and 511, respectively. To evaluate the effects of nafazatrom, LY150310, LY189332, and LY135305 on animal survival, these compounds were given at the maximum anti-metastatic dose of 200, 60, 20, and 6 mg/kg/day, respectively. Two dosing schedules were used: (a) from day 5 to 19; (b) from day 5 to death. These compounds did not significantly alter median survival times or the number of long-term survivors at any dosing schedule. RA233 did not inhibit lung metastasis or increase median survival time at a schedule in which the maximum tolerated dose of 200 mg/kg/day was given until death on day 5. Postmortem examination of animals given nafazatrom, LY150310, LY189332, and LY1350310 revealed complete suppression of lung lesions, whereas lesions developed in the liver, kidney, spleen, and brain. The results of this study suggest that the effects of a compound on the number of metastatic lesions in target organs may not be predictive of its effects on survival. To successfully translate laboratory data into clinical applications, survival should be considered a predictor of the potential clinical utility of a compound.
    LY150310 free base

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