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tumor+xenograft+model

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製品番号 製品名 Target 研究分野 構造式
  • HY-164388
    Z-VAD
    15+ Cited Publications

    Caspase Apoptosis Autophagy Necroptosis Cardiovascular Disease Cancer
    Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
    Z-VAD
  • HY-100591
    SirReal2
    2 Publications Verification

    Sirtuin Neurological Disease Inflammation/Immunology Cancer
    SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
    SirReal2
  • HY-151462
    RP-6685
    3 Publications Verification

    DNA/RNA Synthesis Cancer
    RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model . RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    RP-6685
  • HY-P991669

    AML-01

    Caspase Apoptosis Cancer
    IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .
    IGN523
  • HY-16999

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
    RO8994
  • HY-P99925

    REGN421

    Notch Metabolic Disease Cancer
    Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
    Enoticumab
  • HY-147208

    YAP Cancer
    MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model .
    MSC-4106
  • 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-106031

    Topoisomerase DNA/RNA Synthesis Cancer
    F-14512 is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 can be used to study breast cancer .
    F-14512
  • HY-168035

    Histone Methyltransferase Cancer
    W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .
    W4275
  • 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-178238

    ADC Payload Topoisomerase Cancer
    LD2-3 is a cytotoxic compound derived from Exatecan (HY-13631), designed to be conjugated with anti-FGFR2b or anti-CEA antibodies to form intact antibody-drug conjugate (ADC) molecules. LD2-3 exhibits a remarkable bystander killing effect: it not only effectively kills FGFR2b-positive tumor cells, but also eliminates surrounding FGFR2b-negative cells in co-culture and mixed tumor xenograft models, thereby inducing complete tumor regression. LD2-3 can be used for anti-tumor research in relevant fields such as gastric cancer and lung cancer .
    LD2-3
  • HY-168950

    Annexin A Cancer
    ANXA3 degrader 1 (Compound 18a5) is a highly selective ANXA3 degrader with cancer cell inhibition activity. ANXA3 degrader 1 displays excellent inhibitory effect in a triple-negative breast cancer (TNBC) tumor xenograft model (TGI=96%) .
    ANXA3 degrader 1
  • HY-176508

    Casein Kinase Cancer
    KDX1381 is a bivalent CK2α inhibitor (IC50: 17 nM, KD: 54 nM). KDX1381 has antitumor activity in mouse 786-O and A375 tumor xenograft models. KDX1381 combined with VEGFR inhibitors or DNA damaging agents enhances antitumor efficacy in mouse hepatocellular carcinoma and glioma models .
    KDX1381
  • HY-103441

    EGFR Cancer
    JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
    JNJ28871063 hydrochloride
  • HY-106777
    Cyclopentenylcytosine
    1 Publications Verification

    CPEC; NSC 375575

    DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis Necroptosis Influenza Virus HSV Infection Cancer
    Cyclopentenylcytosine (CPEC), a carbocyclic nucleoside analog of cytosine, is a potent inhibitor of CTP synthetase and causes depletion of CTP and dCTP pools. Cyclopentenylcytosine shows broad-spectrum (both DNA and RNA viruses) antiviral activity. Cyclopentenyl cytosine increases Gemcitabine (HY-17026) radiosensitisation in human pancreatic cancer cells. Cyclopentenylcytosine shows effective antiviral activity in the Ad5/NZW rabbit ocular replication model and shows anti-tumor activity in various tumor xenografts model. Cyclopentenylcytosine can be used for the study of infection and cancer .
    Cyclopentenylcytosine
  • HY-177332

    TAM Receptor SARS-CoV Akt Infection Cancer
    SLC-391 is an orally active AXL kinase inhibitor with an IC50 of 9.6 nM against AXL kinase. SLC-391 inhibits Gas6-induced AXL-dependent phosphorylation of Akt. SLC-391 inhibits SARS-CoV-2 infection, entry and replication in cells. SLC-391 suppresses cancer cell proliferation. SLC-391 inhibits tumor growth in mouse solid tumor xenograft models. SLC-391 can be used for the research of COVID-19, influenza virus infection, triple-negative breast cancer, chronic myeloid leukemia and non-small cell lung cancer .
    SLC-391
  • HY-P10759

    Peptide-Drug Conjugates (PDCs) Aminopeptidase Cancer
    DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
    DTS-201 sodium
  • HY-106603

    Diarylsulfonylurea; LY186641

    Calcium Channel Cancer
    Sulofenur (LY186641) is an orally active anti-tumor agent. Sulofenur induces gene expression through calcium ion-dependent pathways and some protein kinase-independent pathways, and its effect is particularly enhanced in H-ras mutant cells. Sulofenur exhibits significant activity in mouse solid tumor models and human tumor xenograft models .
    Sulofenur
  • HY-103043

    Others Cancer
    Pz 285 is an anti-cancer agent. Pz 285 shows significant inhibitory effect on the viability of MDA-MB-231 breast cancer cells, with an IC50 of 15.0 μM. Pz 285 exhibits remarkable antitumor effects in the mouse tumor xenograft model constructed with highly lung-metastatic MDA-MB-231 LM24 Her2+ breast cancer cells. Pz 285 can be used for the study of breast cancer, especially metastatic breast cancer .
    Pz 285
  • HY-P991561

    CD47 Cancer
    AO-176 is a humanized anti-CD47 IgG2 monoclonal antibody. AO-176 induces tumor phagocytosis through blocking the CD47-SIRPα interaction. AO-176 preferentially binds to tumor versus normal cells and directly kills tumor by a cell autonomous mechanism not ADCC (antibody-dependent cell-mediated cytotoxicity). AO-176 demonstrates dose-dependent antitumor activity in tumor xenograft models. AO-176 can be used for the researches of cancer, such as lymphoma .
    AO-176
  • HY-N2199

    Apoptosis Autophagy PI3K JNK mTOR p38 MAPK CDK MMP TGF-beta/Smad STAT β-catenin Reactive Oxygen Species (ROS) Bcl-2 Family Caspase Inflammation/Immunology Cancer
    Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease .
    Sotetsuflavone
  • HY-P991547

    CD20 Apoptosis Inflammation/Immunology Cancer
    Anti-CD20 Antibody (mAb 1.5.3) is a fully human IgG1 anti-CD20 antibody. Anti-CD20 Antibody (mAb 1.5.3) evokes enhanced pro-apoptotic activity in vitro. Anti-CD20 Antibody (mAb 1.5.3) mediated both complement-dependent cytotoxicity and antibody-dependent cellular cytotoxicity. Anti-CD20 Antibody (mAb 1.5.3) demonstrates enhanced anti-tumor activity in various tumor xenograft models. Anti-CD20 Antibody (mAb 1.5.3) produces a superior B-cell depletion profile in lymph node organs and bone marrow in a primate pharmacodynamic model. Anti-CD20 Antibody (mAb 1.5.3) can be studied in research for B-cell maglignancies .
    Anti-CD20 Antibody (mAb 1.5.3)
  • HY-118269

    c-Met/HGFR Cancer
    OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated .
    OSI-296
  • 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-146780

    TGF-β Receptor Cancer
    TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model .
    TGFβRI-IN-4
  • HY-106154

    Peptide-Drug Conjugates (PDCs) Aminopeptidase Cancer
    DTS-201 (CPI-0004) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
    DTS-201
  • HY-149081

    Estrogen Receptor/ERR Cytochrome P450 Cancer
    ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .
    ERα degrader 6
  • HY-400685

    Drug Intermediate Cancer
    SMD-3040 intermediate-2 is an intermediate in the synthesis of SMD-3040 (HY-156568). SMD-3040 contains SMARCA2/4 ligands, linker and VHL ligands and is a selective SMARCA2 degrader. MD-3040 can be used for ADC drug synthesis and has strong tumor growth inhibition in tumor xenograft models .
    SMD-3040 intermediate-2
  • HY-115908

    CDK Apoptosis Cancer
    ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model .
    ZDLD13
  • HY-173065

    CDK Apoptosis Cancer
    CDK9-IN-36 (Compound T7) is a potent, selective and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. CDK9-IN-36 effectively suppresses cell proliferation, reduces colony formation, and induces apoptosis in Osimertinib (HY-15772)-resistant NSCLC cells by downregulating Mcl-1. CDK9-IN-36 also demonstrates antitumor efficacy in a tumor xenograft model .
    CDK9-IN-36
  • HY-106963

    LGD1550

    RAR/RXR Cancer
    ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
    ALRT1550
  • HY-106031A

    Topoisomerase DNA/RNA Synthesis Cancer
    F-14512 hydrochloride is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 hydrochloride enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 hydrochloride exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 hydrochloride demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 hydrochloride could be used to study breast cancer .
    F-14512 hydrochloride
  • HY-117707

    Raf Cancer
    EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
    EBI-907
  • HY-P992372

    Drug Derivative Transmembrane Glycoprotein Cancer
    huAA98 is a humanized monoclonal antibody and also a CD146 inhibitor. huAA98 binds to human CD146, regulates its activity and inhibits cancer-related angiogenesis, as well as tube formation, motility, proliferation and migration of endothelial cells. huAA98 inhibits angiogenesis in the chick chorioallantoic membrane assay and reduces microvessel density in human tumor xenograft models. huAA98 shows immunoreactivity only to neovascular vessels within tumors and inhibits the growth of tumor xenograft models. huAA98 can be used in studies related to cancer-related angiogenesis, liver cancer, leiomyosarcoma and pancreatic cancer .
    huAA98
  • HY-100591R

    Sirtuin Reference Standards Neurological Disease Inflammation/Immunology Cancer
    SirReal2 (Standard) is the analytical standard of SirReal2 (HY-100591). This product is intended for research and analytical applications. SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
    SirReal2 (Standard)
  • HY-159803

    6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin

    Endogenous Metabolite Cancer
    IST-622 (6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin) is an anti-tumor agent with significant growth inhibitory activity. IST-622 exhibits significant anti-tumor effects against a variety of mouse tumors such as P388 and L1210 leukemias, B16 melanoma, Lewis lung carcinoma, Colon 26 and Colon 38 adenocarcinomas, and M5076 reticulum cell sarcoma. IST-622 was orally administered and the results showed efficacy in different tumor types. In addition, IST-622 provided significant inhibitory effects against two human tumor xenograft models: large cell lung carcinoma (Lu-116) and gastric adenocarcinoma (St-4). IST-622 also exhibited significant growth inhibitory activity against P388 leukemia in vitro, with a half inhibitory concentration (IC50) more than 20 times lower than CT .
    IST-622

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