Search Result
Results for "
gemcitabine
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-17026
-
Gemcitabine
Maximum Cited Publications
266 Publications Verification
LY 188011
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Autophagy
Apoptosis
p38 MAPK
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Infection
Inflammation/Immunology
Cancer
|
|
Gemcitabine (LY 188011) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, and can modulate autophagy. Gemcitabine induces apoptosis through the activation of p38 MAPK. Gemcitabine demonstrates efficacy in mouse models of pancreatic and breast cancer. Gemcitabine can be used for cancer research, such as pancreatic cancer, non-small cell lung cancer, and breast cancer .
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-
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- HY-B0003
-
-
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- HY-160818
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MC3138
2 Publications Verification
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Sirtuin
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Cancer
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MC3138 is a selective SIRT5 activator. MC3138 has antitumor activity on human PDAC cells, with IC50 values of 25.4-236.9 μM. MC3138 combined with Gemcitabine (HY-17026) significantly inhibits tumor growth in mice .
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- HY-13538
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-
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- HY-138253
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dFdU; 2',2'-Difluoro-2'-deoxyuridine
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Drug Metabolite
Apoptosis
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Cancer
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2’,2’-Difluorodeoxyuridine (dFdU) is the main metabolite of Gemcitabine (HY-17026). 2’,2’-Difluorodeoxyuridine causes a concentration- and schedule- dependent radiosensitising effect in vitro. 2’,2’-Difluorodeoxyuridine arrests cell cycle at the early S phase and induces apoptosis in cancer cells .
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-
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- HY-100885
-
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NUC-1031
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DNA/RNA Synthesis
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Cancer
|
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Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.
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-
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- HY-10032
-
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PF 00477736
|
Checkpoint Kinase (Chk)
VEGFR
Src
c-Fms
Aurora Kinase
FGFR
FLT3
RET
CDK
|
Cancer
|
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PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo .
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-
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- HY-P9964
-
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11F8; IMC-11F8; LY3012211
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EGFR
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Cancer
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Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
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- HY-17026R
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-
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- HY-17026E
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dFdCTP trisodium
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Drug Metabolite
DNA/RNA Synthesis
Apoptosis
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Cancer
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Gemcitabine triphosphate (dFdCTP) trisodium is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate trisodium cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate trisodium shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate trisodium partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate trisodium disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate trisodium can be used for the research of pancreatic cancer and non-small cell lung cancer .
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-
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- HY-13672
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-
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- HY-108932
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gemcitabine 5′-phosphate
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Apoptosis
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Cancer
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Gemcitabine monophosphate (Gemcitabine 5′-phosphate) is one of the active intermediates of Gemcitabine (HY-17026). Gemcitabine monophosphate has a synergistic anti-cancer effect and can be delivered by formulating it into nanoparticles .
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- HY-13561
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M475271
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Src
Apoptosis
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Cancer
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AZM475271 (M475271) is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC50s = 0.01, 0.03, 0.08 μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro and in vivo, and reduces microvessel density (MVD). AZM475271 inhibits tumor growth and metastasis. AZM475271 sensitizes tumor cells to the cytotoxic effects of Gemcitabine (HY-17026) .
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- HY-B0003S
-
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LY 188011-13C,15N2 hydrochloride
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Apoptosis
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Autophagy
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Cancer
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Gemcitabine- 13C, 15N2 (hydrochloride) is the 13C and 15N labeled Gemcitabine hydrochloride . Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis .
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- HY-16511
-
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WX-671
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PAI-1
Ser/Thr Protease
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Infection
Cancer
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Upamostat (WX-671), a prodrug of WX-UK1, is an orally active serine protease inhibitor. Upamostat inhibits the urokinase-type plasminogen activator (uPA) system, blocking the plasminogen activation process mediated by it, thereby suppressing the invasion, migration and metastasis of tumor cells. Upamostat can be used in the research of metastatic breast cancer and locally advanced pancreatic cancer .
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- HY-N3387
-
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Apoptosis
NF-κB
Akt
MMP
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Inflammation/Immunology
Cancer
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Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer . Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect . Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo . Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations .
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- HY-17026A
-
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dFdCTP
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Drug Metabolite
DNA/RNA Synthesis
Apoptosis
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Cancer
|
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Gemcitabine triphosphate (dFdCTP) is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate can be used for the research of pancreatic cancer and non-small cell lung cancer .
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- HY-130812
-
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Drug-Linker Conjugates for ADC
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Cancer
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Gemcitabine-O-Si(di-iso)-O-Mc is a agent-linker conjugate for ADC with potent antitumor activity by using Gemcitabine (a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent; HY-17026), linked via the ADC linker .
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- HY-P99667
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OMP-54F28; FZD8-Fc
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Wnt
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Cancer
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Ipafricept (OMP-54F28; FZD8-Fc) is a first class recombinant fusion protein with the extracellular part of the human frizzled-8 receptor fused to a human IgG1 Fc fragment that binds Wnt ligands, which blocks Wnt signaling. Ipafricept reduces tumor growth and results in a decrease in both liver and lung metastases combined with Gemcitabine (HY-17026) in pancreatic cancer mouse models. Ipafricept shows solid tumor inhibition activity with well tolerance, such as desmoid tumor, germ cell cancer, ovarian cancer .
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- HY-138253R
-
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dFdU (Standard); 2',2'-Difluoro-2'-deoxyuridine (Standard)
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Drug Metabolite
Reference Standards
Apoptosis
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Cancer
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2′,2′-Difluorodeoxyuridine (Standard) is the analytical standard of 2′,2′-Difluorodeoxyuridine. This product is intended for research and analytical applications. 2’,2’-Difluorodeoxyuridine (dFdU) is the main metabolite of Gemcitabine (HY-17026). 2’,2’-Difluorodeoxyuridine causes a concentration- and schedule- dependent radiosensitising effect in vitro. 2’,2’-Difluorodeoxyuridine arrests cell cycle at the early S phase and induces apoptosis in cancer cells.
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- HY-138253S
-
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dFdU-13C,15N2; 2',2'-Difluoro-2'-deoxyuridine-13C,15N2
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Isotope-Labeled Compounds
Drug Metabolite
Apoptosis
|
Others
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2′,2′-Difluorodeoxyuridine- 13C, 15N2 (dFdU- 13C, 15N2) is a 13C- and 15N-labeled compound. 2’,2’-Difluorodeoxyuridine (dFdU) is the main metabolite of Gemcitabine (HY-17026). 2’,2’-Difluorodeoxyuridine causes a concentration- and schedule- dependent radiosensitising effect in vitro. 2’,2’-Difluorodeoxyuridine arrests cell cycle at the early S phase and induces apoptosis in cancer cells .
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- HY-113314
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Endogenous Metabolite
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Cancer
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AFMK, antioxidant metabolite of Melatonin, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. AFMK is a poorer scavenger. The pKa of AFMK at physiological pH is 8.7. Antioxidant capacity . AFMK improves the anti-tumor effect of Gemcitabine in PANC-1 cells through the modulation of apoptotic pathway .
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- HY-130818
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ADC Linker
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Cancer
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N-(5-Hydroxypentyl)maleimide is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs), such as Gemcitabine-O-Si(di-iso)-O-Mc (HY-130812) ) .
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- HY-100195
-
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Checkpoint Kinase (Chk)
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Cancer
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SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents .
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- HY-171414
-
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Antibiotic
Bacterial
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Infection
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MC-VC-PAB-O-Gemcitabine is a linker-antibiotic intermediate, which is part of the antibody-antibiotic conjugate (AAC) molecule. MC-VC-PAB-O-Gemcitabine is conjugated with the linker and the antibiotic Gemcitabine (HY-17026). MC-VC-PAB-O-Gemcitabine can be used to study the immunotherapy of bacterial infections and the development of new antibacterial drugs .
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- HY-15883
-
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
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GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 μM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. Gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .
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- HY-13538A
-
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CP-4126 hydrochloride; CO-101 hydrochloride; gemcitabine 5'-elaidate hydrochloride
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Nucleoside Antimetabolite/Analog
Autophagy
Apoptosis
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Cancer
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Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-agent of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate hydrochloride exhibits anti-tumor activity .
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- HY-156027
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- HY-B0003R
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LY 188011 hydrochloride (Standard)
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Reference Standards
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
Autophagy
Apoptosis
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Cancer
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Gemcitabine (hydrochloride) (Standard) is the analytical standard of Gemcitabine (hydrochloride). This product is intended for research and analytical applications. Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis .
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- HY-B0003AS
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- HY-100709
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-
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- HY-16138
-
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CG-200745
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HDAC
MDM-2/p53
Apoptosis
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Cancer
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Ivaltinostat (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat induces apoptosis and has anti-tumour effects .
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- HY-16138A
-
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CG-200745 formic
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HDAC
MDM-2/p53
Apoptosis
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Inflammation/Immunology
Endocrinology
Cancer
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Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic inhibits deacetylation of histone H3 and tubulin. Ivaltinostat formic induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat formic induces apoptosis and has anti-tumour effects .
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- HY-115528
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Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
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Cancer
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FF-10502, a structural analog of Gemcitabine, is a pyrimidine nucleoside antimetabolite. FF-10502 inhibits DNA polymerase α and β. FF-10502 shows beneficial anticancer activity via a mechanism of action on dormant cells .
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- HY-108932A
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gemcitabine 5′-phosphate disodium
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Apoptosis
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Cancer
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Gemcitabine monophosphate (Gemcitabine 5′-phosphate) is one of the active intermediates of Gemcitabine (HY-17026). Gemcitabine monophosphate has a synergistic anti-cancer effect and can be delivered by formulating it into nanoparticles .
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- HY-106777
-
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CPEC; NSC 375575
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DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
Apoptosis
Necroptosis
Influenza Virus
HSV
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Infection
Cancer
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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 .
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- HY-139901
-
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Checkpoint Kinase (Chk)
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Cancer
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Chk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC50 of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma .
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- HY-103367
-
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Checkpoint Kinase (Chk)
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Cancer
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CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer .
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- HY-174448
-
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Wee1
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Cancer
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WEE1-IN-12 (Compound 87) is a Wee1 kinase inhibitor with an IC50 of 2.0 nM. WEE1-IN-12 can inhibit the proliferation of HT29 cells (IC50: 1.07 μM), and when used in combination with Gemcitabine (HY-17026), the effect is better (IC50: 0.34 μM). WEE1-IN-12 can be used in the research of tumors such as colon cancer .
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- HY-B0003A
-
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1'-epi LY 188011 hydrochloride
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Nucleoside Antimetabolite/Analog
Apoptosis
DNA/RNA Synthesis
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Cancer
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1'-epi Gemcitabine hydrochloride is the isomer of Gemcitabine hydrochloride (HY-B0003), and can be used as an experimental control. Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis .
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- HY-17026S
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-
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- HY-178021
-
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HDAC
DNA/RNA Synthesis
Apoptosis
RAD51
Caspase
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Cancer
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HDAC1-IN-11 (Compound 6) is a HDAC1 inhibitor with an IC50 of 106.6 nM. HDAC1-IN-11 inhibits the expression of Sp1 and RAD51, thereby inducing Caspase-dependent apoptosis. HDAC1-IN-11 has antitumor activity and sensitizes Etoposide (HY-13629) and Gemcitabine (HY-17026), promoting synergistic death of NSCLC cells through the inhibition of homologous recombination and non-homologous end joining (NHEJ) pathways involved in DNA DSB repair. HDAC1-IN-11 can be used for chemotherapy of cancers like NSCLC research .
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- HY-178022
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HDAC
Apoptosis
Caspase
RAD51
DNA/RNA Synthesis
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Cancer
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HDAC6-IN-63 (Compound 7) is an orally active HDAC6 inhibitor with an IC50 of 145 nM. HDAC6-IN-63 inhibits the expression of Sp1 and RAD51, thereby inducing Caspase-dependent apoptosis. HDAC6-IN-63 has antitumor activity and sensitizes Etoposide (HY-13629) and Gemcitabine (HY-17026), promoting synergistic death of NSCLC cells through the inhibition of homologous recombination and non-homologous end joining (NHEJ) pathways involved in DNA DSB repair. HDAC6-IN-63 can be used for chemotherapy of cancers like NSCLC research .
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- HY-178293
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Drug-Linker Conjugates for ADC
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Cancer
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N-Succinimidyl 3-maleimidopropionate (Compound MC1) is a Glucuronide-Gemcitabine conjugate. N-Succinimidyl 3-maleimidopropionate can be used to synthesize ADCs (such as cAc10ec-MC1). N-Succinimidyl 3-maleimidopropionate can be used in Hodgkin's lymphoma research .
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- HY-161383
-
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Checkpoint Kinase (Chk)
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Cancer
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CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026) .
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- HY-15882
-
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Endogenous Metabolite
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Cancer
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GNE-783 is a selective CHK1 inhibitor that enhances the activity of gemcitabine. GNE-783 improves the efficacy of anti-metabolite DNA damage drugs by inactivating S-phase and G2-phase cell cycle checkpoints following DNA damage. GNE-783 selectively enhances the chemical synergy of certain drugs in different tumor types, for example, enhancing the activity of temozolomide only in melanoma cell lines .
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- HY-155222
-
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Epigenetic Reader Domain
HDAC
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Cancer
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TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026) .
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- HY-W766239
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-
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- HY-167855S
-
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Isotope-Labeled Compounds
P2Y Receptor
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Inflammation/Immunology
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1’-Epi Gemcitabine hydrochloride- 13C, 15N2 is the 13C- and 15N-labeled MRS4833 (HY-167855). MRS4833 (compound 15) is an orally active, potent, competitive P2Y14R antagonist with an of IC50 of 5.92 nM for hP2Y14R and an IC50 of 4.8 nM for mP2Y14R. MRS4833 reduces airway eosinophilia in a protease-mediated asthma model and reverses chronic neuropathic pain in a mouse CCI model .
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- HY-178451
-
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Apoptosis
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Cancer
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NQO1-responsive prodrug is a prodrug of Gemcitabine (dFdC) (HY-17026) with anti-cancer effect. NQO1-responsive prodrug remains stable in plasma and liver/intestinal S9 fractions, releasing dFdC in an NQO1-dependent manner. NQO1-responsive prodrug induces S-phase arrest and apoptosis. NQO1-responsive prodrug inhibits tumor growth in an A549 xenograft mouse model. NQO1-responsive prodrug can be used for breast and non-small cell lung cancer (NSCLC) research .
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- HY-149050
-
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Influenza Virus
SARS-CoV
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Infection
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Viral polymerase-IN-1 hydrochloride, a Gemcitabine (HY-17026) derivative, potently inhibits influenza A and B viruses infection with IC90 values of 11.4-15.9 μM. Viral polymerase-IN-1 hydrochloride is active against SARS-CoV-2 infection. Viral polymerase-IN-1 hydrochloride suppresses influenza virus infection by affecting viral RNA replication/transcription in cells .
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- HY-146540
-
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HIF/HIF Prolyl-Hydroxylase
Apoptosis
MDM-2/p53
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Cancer
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GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth .
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- HY-154842
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- HY-159577
-
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PI3K
mTOR
Akt
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Cancer
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Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine .
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- HY-123597
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DDUG; NCI C04808
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Autophagy
Checkpoint Kinase (Chk)
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Cancer
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NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
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- HY-145441
-
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Drug Derivative
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Cancer
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GEM–IB is the conjugate of gemcitabine (GEM)-5'-phosphate with ibandronate (IB). GEM–IB as a single agent or in combination with Docetaxel (DTX) demonstrates reduced tumor burden, preservation of the bone architecture, and improved the survival in a murine model of osteosarcoma (OS) .
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- HY-145314
-
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Integrin
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Cancer
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TC113 is a c(RGDyK)-Based conjugate of Gemcitabine (GEM). TC113 could be internalized by A549 cells through integrin αvβ3. TC113 shows potent antiproliferative properties against WM266.4 and A549 cells .
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- HY-163323
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Aldose Reductase
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Cancer
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AKR1C3-IN-12 (compound 2j) is an aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 27 nM. AKR1C3-IN-12 enhances the efficacy of Gemcitabine and Cisplatin in bladder cancer .
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- HY-124731
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-
- HY-108932R
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|
gemcitabine 5′-phosphate (Standard)
|
Reference Standards
Apoptosis
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Cancer
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Gemcitabine monophosphate (Standard) is the analytical standard of Gemcitabine monophosphate (HY-108932). This product is intended for research and analytical applications. Gemcitabine monophosphate (Gemcitabine 5′-phosphate) is one of the active intermediates of Gemcitabine (HY-17026). Gemcitabine monophosphate has a synergistic anti-cancer effect and can be delivered by formulating it into nanoparticles .
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- HY-179217
-
|
|
JNK
Apoptosis
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Cancer
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|
GSTP1/M2-IN-1 is a GSTP1/GSTM2 inhibitor(IC50 = 1.56 μM/0.09 μM). GSTP1/M2-IN-1 can activate the JNK pathway and induce cell apoptosis. GSTP1/M2-IN-1 can be used for the study of breast cancer and pancreatic cancer .
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- HY-129085
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C5OH
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Drug Derivative
Apoptosis
NF-κB
|
Cancer
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5-Methyl cromolyn (C5OH) disodium, an analog of Cromolyn (HY-B1619), is a S100P inhibitor. 5-Methyl cromolyn disodium inhibits the binding of S100P to its receptor RAGE, NF-κB activity and cell proliferation, and promotes Gemcitabine (HY-17026)-induced apoptosis. 5-Methyl cromolyn disodium reduces tumor growth and metastasis, and prolongs survival in mouse models of syngeneic PDAC. 5-Methyl cromolyn disodium can be used for pancreatic cancer like pancreatic ductal adenocarcinoma (PDAC) research .
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- HY-169006
-
|
|
Apoptosis
PKC
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Cancer
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|
Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model .
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- HY-10032R
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|
PF 00477736 (Standard)
|
Checkpoint Kinase (Chk)
Reference Standards
VEGFR
Src
c-Fms
Aurora Kinase
FGFR
FLT3
RET
CDK
|
Cancer
|
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PF 477736 (Standard) is the analytical standard of PF 477736 (HY-10032). This product is intended for research and analytical applications. PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo .
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- HY-182898
-
|
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Apoptosis
Glycosidase
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Inflammation/Immunology
|
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Gal-dMor-Gem is a selective senescent cell scavenger, Apoptosis inducer, and a prodrug of Gemcitabine (HY-17026). Gal-dMor-Gem releases Gemcitabine upon activation by Esterases and β-gal. Gal-dMor-Gem reduces SA-β-gal, preferentially induces apoptosis in senescent cells, regulates apoptosis-related proteins, accumulates in senescent tissues, and ameliorates senescence-related organ phenotypes. Gal-dMor-Gem is applicable to research on chemotherapy-induced senescence .
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- HY-P991883
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|
Licartin; Metuximab; Mehuzumab
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Apoptosis
CDK
Caspase
Bcl-2 Family
|
Cancer
|
|
Metuzumab (Licartin) is a human-mouse chimeric IgG1 monoclonal antibody targeting CD147. Metuzumab induces Apoptosis, reduces levels of Cyclin D1, full-length Caspase-3, and Bcl-2, and increases Bax expression. Metuzumab enhances the sensitivity of non-small cell lung cancer (NSCLC) cells to Gemcitabine (HY-17026). Metuzumab is applicable for research on hepatocellular carcinoma and non-small cell lung cancer [1] [2].
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-
- HY-114563
-
|
dFdG
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Drug Derivative
|
Cancer
|
|
LY 223592 (Compound I-a) is a Gemcitabine (HY-17026) derivative. LY 223592 has the biological activity of highly selective inhibition of lung cancer cell proliferation (IC50 = 5.6 nM in A549 cells) and low cytotoxicity to normal cells. LY 223592 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
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- HY-185323
-
|
|
Drug Derivative
Apoptosis
DNA/RNA Synthesis
|
Neurological Disease
Cancer
|
|
Gem-C12 is a prodrug of Gemcitabine (HY-17026). Gem-C12 terminates DNA chain elongation, inhibits nucleic acid synthesis and induces Apoptosis. Gem-C12 inhibits the proliferation of glioma cells. Gem-C12 and Honokiol (HY-N0003) exhibit synergistic anti-glioblastoma activity. Gem-C12 can be used in research related to glioblastoma multiforme .
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-
- HY-176957
-
|
|
Wee1
|
Cancer
|
|
PKMYT1-IN-11 (Example 1) is a PKMYT1 inhibitor with an IC50 of 4.49 nM. PKMYT1-IN-11 inhibits the proliferation of HCC1569 cells. When combined with Gemcitabine (HY-17026), PKMYT1-IN-11 shows a significant anti-tumor effect in the OVCAR3 xenograft mouse model. PKMYT1-IN-11 can be used for the study of various cancers such as breast cancer and ovarian cancer .
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-
- HY-16512
-
|
WX-671 hydrogen sulfate
|
PAI-1
Ser/Thr Protease
|
Cancer
|
|
Upamostat (WX-671) hydrogen sulfate, a prodrug of WX-UK1 (HY-100415), is an orally active serine protease inhibitor. Upamostat hydrogen sulfate inhibits the urokinase-type plasminogen activator (uPA) system, blocking the plasminogen activation process mediated by it, thereby suppressing the invasion, migration and metastasis of tumor cells. Upamostat hydrogen sulfate can be used in the research of metastatic breast cancer and locally advanced pancreatic cancer .
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-
- HY-120825
-
|
|
Apoptosis
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Keap1-Nrf2
|
Cancer
|
|
QD 232 is a quinazolinedione-based ROS inducer and an apoptosis inducer with cytotoxicity and redox regulatory activity. QD 232 promotes ROS accumulation, activates the NRF2-mediated oxidative stress response and unfolded protein response pathways, and upregulates downstream antioxidant and stress response genes. QD 232 inhibits mtDNA transcription driven by HSP2 and LSP promoters, and impairs mitochondrial oxidative phosphorylation function. QD 232 induces apoptosis of pancreatic ductal adenocarcinoma cells and exerts cytotoxicity against gemcitabine (HY-17026)-resistant pancreatic ductal adenocarcinoma cells. QD 232 delays tumor growth in a mouse pancreatic cancer xenograft model .
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- HY-P11781
-
|
|
Drug Derivative
|
Cancer
|
|
HW12 is a random peptide containing an N-terminal cysteine and is not an EGFR ligand. HW12 can serve as a control for GE11 (HY-P10128)-conjugated mixed micelles targeting EGFR. HW12 is applicable to pancreatic cancer-related research .
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-
| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P11781
-
|
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Drug Derivative
|
Cancer
|
|
HW12 is a random peptide containing an N-terminal cysteine and is not an EGFR ligand. HW12 can serve as a control for GE11 (HY-P10128)-conjugated mixed micelles targeting EGFR. HW12 is applicable to pancreatic cancer-related research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P9964
-
|
11F8; IMC-11F8; LY3012211
|
EGFR
|
Cancer
|
|
Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
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-
(5)
-
- HY-P99667
-
|
OMP-54F28; FZD8-Fc
|
Wnt
|
Cancer
|
|
Ipafricept (OMP-54F28; FZD8-Fc) is a first class recombinant fusion protein with the extracellular part of the human frizzled-8 receptor fused to a human IgG1 Fc fragment that binds Wnt ligands, which blocks Wnt signaling. Ipafricept reduces tumor growth and results in a decrease in both liver and lung metastases combined with Gemcitabine (HY-17026) in pancreatic cancer mouse models. Ipafricept shows solid tumor inhibition activity with well tolerance, such as desmoid tumor, germ cell cancer, ovarian cancer .
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-
(5)
-
- HY-P991883
-
|
Licartin; Metuximab; Mehuzumab
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Apoptosis
CDK
Caspase
Bcl-2 Family
|
Cancer
|
|
Metuzumab (Licartin) is a human-mouse chimeric IgG1 monoclonal antibody targeting CD147. Metuzumab induces Apoptosis, reduces levels of Cyclin D1, full-length Caspase-3, and Bcl-2, and increases Bax expression. Metuzumab enhances the sensitivity of non-small cell lung cancer (NSCLC) cells to Gemcitabine (HY-17026). Metuzumab is applicable for research on hepatocellular carcinoma and non-small cell lung cancer [1] [2].
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-17026E
-
|
dFdCTP trisodium
|
Structural Classification
Natural Products
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Source Classification
Cancer
|
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
|
Gemcitabine triphosphate (dFdCTP) trisodium is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate trisodium cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate trisodium shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate trisodium partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate trisodium disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate trisodium can be used for the research of pancreatic cancer and non-small cell lung cancer .
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-
-
- HY-N3387
-
-
-
- HY-17026A
-
|
dFdCTP
|
Structural Classification
Natural Products
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Source Classification
Cancer
|
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
|
Gemcitabine triphosphate (dFdCTP) is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate can be used for the research of pancreatic cancer and non-small cell lung cancer .
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-
-
- HY-113314
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0003S
-
|
|
|
Gemcitabine- 13C, 15N2 (hydrochloride) is the 13C and 15N labeled Gemcitabine hydrochloride . Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis .
|
-
-
- HY-138253S
-
|
|
|
2′,2′-Difluorodeoxyuridine- 13C, 15N2 (dFdU- 13C, 15N2) is a 13C- and 15N-labeled compound. 2’,2’-Difluorodeoxyuridine (dFdU) is the main metabolite of Gemcitabine (HY-17026). 2’,2’-Difluorodeoxyuridine causes a concentration- and schedule- dependent radiosensitising effect in vitro. 2’,2’-Difluorodeoxyuridine arrests cell cycle at the early S phase and induces apoptosis in cancer cells .
|
-
-
- HY-B0003AS
-
|
|
|
(2S)-Gemcitabine- 13C, 15N2 (hydrochloride) is the 13C and 15N labeled (2S)-Gemcitabine hydrochloride .
|
-
-
- HY-17026S
-
|
|
|
antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, resulting in autophagyand apoptosis .
|
-
-
- HY-W766239
-
|
|
|
1'-Epi Gemcitabine-3',5'-Dibenzoate- 13C, 15N2 is the 13C- and 15N-labeled 1'-Epi Gemcitabine-3',5'-Dibenzoate.
|
-
-
- HY-167855S
-
|
|
|
1’-Epi Gemcitabine hydrochloride- 13C, 15N2 is the 13C- and 15N-labeled MRS4833 (HY-167855). MRS4833 (compound 15) is an orally active, potent, competitive P2Y14R antagonist with an of IC50 of 5.92 nM for hP2Y14R and an IC50 of 4.8 nM for mP2Y14R. MRS4833 reduces airway eosinophilia in a protease-mediated asthma model and reverses chronic neuropathic pain in a mouse CCI model .
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