Search Result
Results for "
cancer prodrug
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0255
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GS 0840
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HBV
Orthopoxvirus
HSV
DNA/RNA Synthesis
ATM/ATR
CDK
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Infection
Cancer
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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 .
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- HY-124584
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Apoptosis
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Cancer
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Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis .
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- HY-120313
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Drug Derivative
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Cancer
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SN23862 is a cancer prodrug with anti-cancer activity, and an analogue of CB-1954 (HY-13543). SN23862 can be used for cancer research .
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- HY-174460
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Drug Intermediate
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Cancer
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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 .
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- HY-176149
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CaMK
MMP
AMPK
Apoptosis
Autophagy
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Cancer
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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 .
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- HY-161687
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Src
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Cancer
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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 .
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- HY-169131
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AMPK
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Cancer
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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 .
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- HY-124584A
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Apoptosis
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Cancer
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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 .
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- HY-114206
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Histone Methyltransferase
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Cancer
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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 .
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- HY-10127A
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AZD1152 dihydrochloride
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Aurora Kinase
Apoptosis
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Cancer
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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 .
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- HY-10127
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Barasertib
Maximum Cited Publications
19 Publications Verification
AZD1152
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Aurora Kinase
Apoptosis
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Cancer
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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 .
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- HY-168903
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STAT
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Cancer
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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 .
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- HY-171030
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Ferroptosis
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Cancer
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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 .
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- HY-136506
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Drug Derivative
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Cancer
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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 .
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- HY-168143
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Histone Methyltransferase
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Cancer
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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. .
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- HY-161089
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Others
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Cancer
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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 .
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- HY-162470
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Aurora Kinase
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Cancer
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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 .
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- HY-149040
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(S)-OBI-3424; (S)-TH-3424; AST-3424
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17β-HSD
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Cancer
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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 .
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- HY-10127R
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AZD1152 (Standard)
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Reference Standards
Aurora Kinase
Apoptosis
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Cancer
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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 .
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- HY-168913
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PSMA
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Cancer
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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 .
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- HY-159924
-
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-P10765
-
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Peptide-Drug Conjugates (PDCs)
Topoisomerase
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Cancer
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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 .
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- HY-177083
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AVA-6000
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FAP
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Cancer
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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) .
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- HY-158331
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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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 .
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- HY-161838
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ATM/ATR
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Cancer
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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.
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- HY-P10759
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Peptide-Drug Conjugates (PDCs)
Aminopeptidase
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Cancer
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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 .
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- HY-P99101
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AEX-4089
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ADC Antibody
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Cancer
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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 .
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- HY-174450
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Epigenetic Reader Domain
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Cancer
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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 .
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- HY-131605
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GCV-TP
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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 .
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- HY-123875A
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EPI-506
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Androgen Receptor
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Cancer
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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 .
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- HY-131605B
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GCV-TP disodium
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CMV
DNA/RNA Synthesis
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Infection
Cancer
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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 .
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- HY-175201
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LPL Receptor
STAT
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Cancer
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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 .
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- HY-144876
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Reactive Oxygen Species (ROS)
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Cancer
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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 .
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- HY-B0255R
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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 .
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- HY-134160
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5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione; 5-Fluorodihydrouracil
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Nucleoside Antimetabolite/Analog
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Cancer
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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.
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-
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- HY-135124
-
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ADC Payload
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Cancer
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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 .
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- HY-135123
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ADC Payload
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Cancer
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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 .
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-
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- HY-N6263
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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 .
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-
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- HY-134160S
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5-DHFU-13C,15N2; 5-Fluorodihydropyrimidine-2,4-dione-13C,15N2; 5-Fluorodihydrouracil-13C,15N2
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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.
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- HY-135125
-
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ADC Payload
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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 .
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- 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 .
|
-
- 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 .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- 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 .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-134160S
-
|
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.
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-
Cat. No. |
Product Name |
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Classification |
-
- HY-175201
-
|
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Azide
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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 .
|
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