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cancer prodrug

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0255
    Adefovir dipivoxil
    1 Publications Verification

    GS 0840

    HBV Orthopoxvirus HSV DNA/RNA Synthesis ATM/ATR CDK Infection Cancer
    Adefovir dipivoxil is an orally active adenosine analog and Adefovir prodrug. Adefovir dipivoxil inhibits DNA synthesis, activates the ATR signaling pathway, and disrupts the KCTD12-CDK1 interaction. Adefovir dipivoxil has antiviral activity against PRV, HBV, and orthopoxviruses. Adefovir dipivoxil has inhibitory effects on both lamivudine-resistant and wild-type strains. Adefovir dipivoxil has antitumor activity against lung and colon cancer .
    Adefovir dipivoxil
  • HY-124584
    Minnelide
    2 Publications Verification

    Apoptosis Cancer
    Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis .
    Minnelide
  • HY-120313

    Drug Derivative Cancer
    SN23862 is a cancer prodrug with anti-cancer activity, and an analogue of CB-1954 (HY-13543). SN23862 can be used for cancer research .
    SN23862
  • HY-174460

    Drug Intermediate Cancer
    pCR8 is a prodrug of CR8 (HY-18340). pCR8 is amphiphilic and can self-assemble into nanoparticles. pCR8 can release CR8 under the action of high concentration of H2O2 in the tumor microenvironment. CR8 is a molecular glue degrader that can effectively degrade cell cycle-related proteins and has antitumor activity. pCR8 can be used in the research of tumors such as breast cancer .
    pCR8
  • HY-176149

    CaMK MMP AMPK Apoptosis Autophagy Cancer
    Fluoxetine-Conjugated Platinum(IV) prodrug-1 (Compound 8) is an eEF2K inhibitor. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits cancer cell proliferation, induces DNA damage, cell cycle arrest at S phase and apoptosis. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces ROS accumulation and mitochondrial dysfunction. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits TNBC cell migration and invasion by inhibiting MMP-2 activity. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces autophagy in TNBC cells by activating AMPK. Fluoxetine-Conjugated Platinum(IV) prodrug-1 has antitumor activity and activates immunosuppression in the 4T1-Luc mouse model. Fluoxetine-Conjugated Platinum(IV) prodrug-1 can be used in triple-negative breast cancer (TNBC) research .
    Fluoxetine-Conjugated Platinum(IV) prodrug-1
  • HY-161687

    Src Cancer
    Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC50s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively .
    Cisplatin/Dasatinib prodrug-1
  • HY-169131

    AMPK Cancer
    ALKBH1-IN-4 prodrug (Compound 29E) is a prodrug of a DNA N6-methyladenine demethylase ALKBH1 inhibitor that significantly increases the abundance of 6mA in cells and upregulates the AMPK signaling pathway, thereby inhibiting the viability of gastric cancer cells. ALKBH1-IN-4 prodrug exhibits excellent cellular activity and favorable metabolic exposure in vivo, and holds promise for research in gastric cancer .
    ALKBH1-IN-3 prodrug
  • HY-124584A

    Apoptosis Cancer
    Minnelide free base is a prodrug of Triptolide (HY-32735) that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide free base promotes apoptosis .
    Minnelide free base
  • HY-114206

    Histone Methyltransferase Cancer
    SKI-73 is a chemical probe for CARM1 with prodrug properties. SKI-73 can rapidly penetrate cell membranes and be processed into active inhibitors. SKI-73 inhibits the invasion of breast cancer cells and can be used in the study of cancer .
    SKI-73
  • HY-10127A

    AZD1152 dihydrochloride

    Aurora Kinase Apoptosis Cancer
    Barasertib (AZD1152 dihydrochloride), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152 dihydrochloride) induces growth arrest and apoptosis in cancer cells .
    Barasertib dihydrochloride
  • HY-10127
    Barasertib
    Maximum Cited Publications
    19 Publications Verification

    AZD1152

    Aurora Kinase Apoptosis Cancer
    Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells .
    Barasertib
  • HY-168903

    STAT Cancer
    STAT3-IN-41 (Compound 16) is a prodrug of compound 1. STAT3-IN-41 slowly releases compound 1 inhibiting STAT3 signaling pathway. STAT3-IN-41 shows antitumor activity against lung cancer, hepatocellular carcinoma and pancreatic cancer .
    STAT3-IN-41
  • HY-171030

    Ferroptosis Cancer
    Pro-GA is a γ-Glutamylcyclotransferase (GGCT) inhibitor and a cell-permeable diester-type pro-drug with anticancer activity, GGCT is a key enzyme in glutathione metabolism and is involved in the ferroptosis pathway. Pro-GA exhibits an IC50 of 57 μM against the bladder cancer cell line T24 and can be utilized in cancer research .
    Pro-GA
  • HY-136506
    NUC-7738
    1 Publications Verification

    Drug Derivative Cancer
    NUC-7738, an aryloxy phosphoramidate of 3′-Deoxyadenosine, is a 5′-aryloxy phosphoramidate prodrug of 3′-Deoxyadenosine (3′-dA). NUC-7738 has potent cytotoxic activity against a panel of hematological cancer cell lines. NUC-7738 can be used in research of cancer .
    NUC-7738
  • HY-168143

    Histone Methyltransferase Cancer
    YD1342 is a prodrug of YD1130, which exhibits potent inhibitory effects on cellular substrate methylation, breast cancer cell clonogenicity, and tumor growth in animal models, exceeding or matching known PRMT4-specific inhibitors. .
    YD1342
  • HY-161089

    Others Cancer
    Antiproliferative agent-45 (compound 9) is a prodrug. Antiproliferative agent-45 exhibits significant anti-proliferative effects for human pancreatic cells in hypoxia but fewer effects in normoxia. Antiproliferative agent-45 can be used for cancer research .
    Antiproliferative agent-45
  • HY-162470

    Aurora Kinase Cancer
    DBPR728 is an acyl prodrug of 6K465 that carries fewer hydrogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465 .
    DBPR728
  • HY-149040

    (S)-OBI-3424; (S)-TH-3424; AST-3424

    17β-HSD Cancer
    Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research .
    Odafosfamide
  • HY-10127R

    AZD1152 (Standard)

    Reference Standards Aurora Kinase Apoptosis Cancer
    Barasertib (Standard) is the analytical standard of Barasertib. This product is intended for research and analytical applications. Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells .
    Barasertib (Standard)
  • HY-168913

    PSMA Cancer
    CTT2274 is a prodrug of MMAE (HY-15162). CTT2274 is composed of a prostate-specific membrane antigen (PSMA)-binding scaffold, a biphenyl motif, a pH-sensitive phosphoramidate linker, and MMAE payload. CTT2274 shows selective binding to PSMA and delivers MMAE. CTT2274 inhibits prostate cancer .
    CTT2274
  • HY-159924

    Opioid Receptor Neurological Disease
    DBPR116 is a prodrug of BPRMU191 (HY-159923) with blood-brain barrier penetration capability. DBPR116 significantly improves the delivery of centrally targeted drugs. In combination with the antagonist Naltrexone (HY-76711), DBPR116 demonstrated superior safety and analgesic efficacy compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a prodrug strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing potential as a safer opioid analgesic .
    DBPR116
  • HY-P10765

    Peptide-Drug Conjugates (PDCs) Topoisomerase Cancer
    DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer .
    DTS-108
  • HY-177083

    AVA-6000

    FAP Cancer
    Faridoxorubicin (AVA-6000) is a prodrug targeting fibroblast activation protein α (FAPα). Faridoxorubicin releases active doxorubicin through FAPα-mediated cleavage, enhancing intratumoral drug exposure and reducing cardiac toxicity. Faridoxorubicin is promising for research of solid tumors (e.g., colorectal cancer liver metastasis) .
    Faridoxorubicin
  • HY-158331

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    Gal-ARV-771, PROTAC prodrug, is a gal modified ARV-771 (HY-100972). Gal-ARV-771 can be activated in SA-β-Gal-expressed cancer senescent cells to release ARV-771. Gal-ARV-771 induces selective degradation of BRD4 protein by the ubiquitin-proteasome pathway in senescent cells. Gal-ARV-771 promotes apoptosis of senescent cancer cells .
    Gal-ARV-771
  • HY-161838

    ATM/ATR Cancer
    ICT10336 is a hypoxia-responsive prodrug of ATR inhibitor, AZD6738 (HY-19323). ICT10336 is hypoxia-activated and specifically releases AZD6738 only in hypoxic conditions in vitro. This can inhibit ATR activation (T1989 and S428 phosphorylation) and subsequently abrogate HIF1a-mediated adaptation of hypoxic cancers cells, thus selectively inducing cell death in 2D and 3D cancer models. ICT10336 is a metabolic substrate of CYPOR activity.
    ICT10336
  • 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-P99101

    AEX-4089

    ADC Antibody Cancer
    Vobramitamab is a humanized B7-H3 monoclonal antibody (mAb). Vobramitamab conjugated with prodrug seco-DUBA (HY-132180A) via a cleavable linker, to form antibody-drug conjugate (ADC), the MGC018. MGC018 displays potent antitumor activity in preclinical tumor models of breast, ovarian, and lung cancer, as well as melanoma .
    Vobramitamab
  • HY-174450

    Epigenetic Reader Domain Cancer
    KMT9-IN-1 (Compound 8) is a KMT9 inhibitor and the ethyl ester prodrug of compound 7b. KMT9-IN-1 releases the active form 7b via esterases in cells. KMT9-IN-1 targets KMT9 in cells and reduces H4K12me1 levels. KMT9-IN-1 has antitumor activity against colon cancer. KMT9-IN-1 can be used in the research of prostate cancer and hepatocellular carcinoma .
    KMT9-IN-1
  • HY-131605

    GCV-TP

    Endogenous Metabolite CMV DNA/RNA Synthesis Infection Cancer
    Ganciclovir triphosphate (GCV-TP) is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate has an IC50 of 0.01 μM against CMV strains from humans, monkeys, mice, and guinea pigs. Ganciclovir triphosphate has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
    Ganciclovir triphosphate
  • HY-123875A

    EPI-506

    Androgen Receptor Cancer
    Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7 .
    Ralaniten triacetate
  • HY-131605B

    GCV-TP disodium

    CMV DNA/RNA Synthesis Infection Cancer
    Ganciclovir triphosphate (GCV-TP) disodium is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate disodium is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate disodium has an IC50 of 0.01 μM against CMV strains from humans, monkeys, mice, and guinea pigs. Ganciclovir triphosphate disodium has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
    Ganciclovir triphosphate disodium
  • HY-175201

    LPL Receptor STAT Cancer
    pro-FTY, a FTY720 (HY-12005) anticancer prodrug, is a sphingosine-1-phosphate (S1P) (HY-108496) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel (HY-B0015) or Doxorubicin (HY-15142A). pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia .
    pro-FTY
  • HY-144876

    Reactive Oxygen Species (ROS) Cancer
    RIDR-PI-103 is a reactive oxygen species (ROS)-induced agent release proagent with a self-cyclizing moiety linked to a pan-PI3K inhibitor (PI-103). Doxorubicin and RIDR-PI-103 shows a synergistic effect in MDA-MB-361 and MDA-MB-231 cells to inhibit cancer cell proliferation .
    RIDR-PI-103
  • HY-B0255R

    GS 0840 (Standard)

    Reference Standards HBV Reverse Transcriptase Orthopoxvirus Endogenous Metabolite Infection Cancer
    Adefovir dipivoxil (Standard) is the analytical standard of Adefovir dipivoxil. This product is intended for research and analytical applications. Adefovir dipivoxil is an orally active adenosine analog and Adefovir prodrug. Adefovir dipivoxil inhibits DNA synthesis, activates the ATR signaling pathway, and disrupts the KCTD12-CDK1 interaction. Adefovir dipivoxil has antiviral activity against PRV, HBV, and orthopoxviruses. Adefovir dipivoxil has inhibitory effects on both lamivudine-resistant and wild-type strains. Adefovir dipivoxil has antitumor activity against lung and colon cancer .
    Adefovir dipivoxil (Standard)
  • HY-134160

    5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione; 5-Fluorodihydrouracil

    Nucleoside Antimetabolite/Analog Cancer
    5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
    5,6-Dihydro-5-Fluorouracil
  • HY-135124

    ADC Payload Cancer
    DC44SMe, a phosphate proagent of cytotoxic DNA alkylator DC44, can be used in the synthesis of antibody-drug conjugate (ADC). DC44SMe exhibits IC50s of 2.0 nM, 2.8 nM, and 1.9 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC44SMe can be used for the targeted treatment of cancer .
    DC44SMe
  • HY-135123

    ADC Payload Cancer
    DC4SMe, a phosphate proagent of cytotoxic DNA alkylator DC4, can be used in the synthesis of antibody-drug conjugate (ADC). DC4SMe exhibits IC50s of 1.9 nM, 2.9 nM, and 1.8 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC4SMe can be used for the targeted treatment of cancer .
    DC4SMe
  • HY-N6263
    EGCG Octaacetate
    1 Publications Verification

    AcEGCG; Peracetylated (-)-epigallocatechin-3-gallate

    Bacterial PI3K Akt NF-κB Infection Inflammation/Immunology Cancer
    EGCG Octaacetate (AcEGCG) is a proagent of Green tea epigallocatechin-3-gallate (EGCG). EGCG Octaacetate decreases the proinflammatory mediator levels by down-regulating of PI3K/Akt/NFκB phosphorylation and p65 acetylation. EGCG octaacetate is the potential antibacterial compound for gram-positive bacteria (GPB) and gram-negative bacteria (GNB). EGCG Octaacetate exhibits antioxidant, anti-angiogenesis, anti-inflammatory and antitumor activities .
    EGCG Octaacetate
  • HY-134160S

    5-DHFU-13C,15N2; 5-Fluorodihydropyrimidine-2,4-dione-13C,15N2; 5-Fluorodihydrouracil-13C,15N2

    Isotope-Labeled Compounds Nucleoside Antimetabolite/Analog Cancer
    5,6-Dihydro-5-Fluorouracil- 13C, 15N2 (5-DHFU- 13C, 15N2) is the 13C- and 15N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
    5,6-Dihydro-5-Fluorouracil-13C,15N2
  • HY-135125

    ADC Payload Cancer
    DC4, an ADC cytotoxin, can be used in the synthesis of antibody-drug conjugate (ADC). DC4 can be used for the targeted treatment of cancer .
    DC4

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