gemcitabine

Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

Gemcitabine hydrochloride (LY 188011 hydrochloride) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

Gemcitabine elaidate (CP-4126), is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.

Gemcitabine elaidate (CP-4126) hydrochloride is a lipophilic pro-drug of Gemcitabine, converted to Gemcitabine by esterases for phosphorylation. Unlike gemcitabine, Gemcitabine elaidate hydrochloride can be administered orally, displaying schedule and dose-dependent toxicity and antitumor activity.

Gemcitabine-O-Si(di-iso)-O-Mc, a drug-linker conjugate for Antibody-Drug Conjugates (ADC), exhibits potent antitumor activity. It incorporates Gemcitabine, a pyrimidine nucleoside analog antimetabolite and antineoplastic agent, connected through the ADC linker [1].

Mc-O-Si(di-iso)-O-Gemcitabine is a thiol-reactive Drug-linker that can be used in the synthesis of antibody-drug conjugates (ADCs).

R306465 is a novel HDAC inhibitor with broad-spectrum antitumor activity against solid (IC50: 30 to 300 nM) and hematological malignancies. R306465 was found to be a potent inhibitor of HDAC1 and -8 (class I) in vitro.

Gemcitabine monophosphate disodium salt is a monophosphate derivative of Gemcitabine.

Gemcitabine triphosphate (dFdCTP), alongside its counterpart, the active diphosphate (dFdCDP), represents one of the two primary nucleoside metabolites of Gemcitabine within cellular structures. It serves as a benchmark in radiolabeled probe imaging investigations aimed at pinpointing tumors responsive to Gemcitabine. Furthermore, it is instrumental in assessing the compound's absorption and retention by cells [1] [2].

Gemcitabine EP Impurity C-13C-15N2 is the 13C and 15N labeled compound of Gemcitabine EP Impurity C.

AFMK (Formyl-N-acetyl-5-methoxykynurenamine) is an active metabolite of Melatonin with antioxidant and free radical scavenging activity. AFMK is a modulator of apoptosis and improves the anti-tumor effect of Gemcitabine in PANC-1 cells.

2'-Deoxycytidine hydrochloride is the hydrochloride form of 2'-Deoxycytidine, an important deoxyribonucleoside analog commonly used in DNA synthesis and potentially anticancer, and its derivative Gemcitabine has been developed as an anticancer drug.2'-Deoxycytidine 2'-Deoxycytidine hydrochloride protects mice from the lethal toxicity of cytosine arabinoside(araC).

LY2334737 is an orally available prodrug of gemcitabine with antineoplastic activity.

GNE-900 is an ATP-competitive ChK1 inhibitor with selective and oral activity.GNE-900 inhibits ChKl and ChK2 with IC50 values of 0.0011 and 1.5 µM, respectively.GNE-900 enhances DNA damage and induces apoptosis. GNE-900 has antitumor activity.

Vactosertib Hydrochloride (EW-7197 Hydrochloride) is an orally active and highly efficient ATP-competitive ALK5 (activin receptor-like kinase 5) inhibitor, a TGF-β receptor I inhibitor with anti-metastatic and anticancer properties. It sensitizes pancreatic cancer cells to gemcitabine by inhibiting their viability.

RX-3117 (fluorocyclopentenylcytosine) is a novel a cytidine analog. RX-3117 displays anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.

Tetrahydrouridine (NSC-112907; THU) is a multidrug resistance modulator. It can be used in cancer treatment to make tumor cells more sensitive to radiation therapy. THU is a competitive cytidine deaminase(CDA) inhibitor that inhibits deamination in the catabolism of cytotoxic deoxycytidine analogs such as ara-C and Gemcitabine.

Troxacitabine, a DNA polymerase inhibitor, is potentially used for the treatment of acute myeloid leukemia (AML). In comparison with gemcitabine, troxacitabine was equally active against MiaPaCa and was more efficacious against Panc-01.

Mc-O-Si(di-iso)-Cl is a cleavable ADC linker, frequently used in the synthesis of antibody-drug conjugates (ADCs) such as Gemcitabine-O-Si(di-iso)-O-Mc [1].

N-(5-Hydroxypentyl)maleimide is a non-cleavable ADC linker used in synthesizing antibody-drug conjugates (ADCs) and is essential in producing the ADC compound Gemcitabine-O-Si(di-iso)-O-Mc [1].

SL-01 is an oral derivative of gemcitabine. SL-01 inhibited human breast cancer growth through the induction of apoptosis. SL-01 inhibited human cancer growth more potently than gemcitabine.

Nic-15 (compound 4n) serves as an anti-constrictive agent targeting the low vascular characteristics of pancreatic tumors. These characteristics enable cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop resistance to treatment. Nic-15 modulates the PI3K Akt mTOR pathway and alleviates ER stress induced by Gemcitabine. It significantly inhibits migration and colony formation in MIA PaCa-2 and PANC-1 pancreatic cancer cells. When used in combination with Gemcitabine, Nic-15 effectively addresses resistance issues in pancreatic tumors. In xenograft models in vivo, Nic-15 notably enhances the efficacy of Gemcitabine.

Pixatimod (also known as PG-545) is a synthetic carbohydrate-modified heparan sulfate mimetic and a Toll-like receptor 9 (TLR9) agonist. It exhibits potential immunostimulatory, antitumor, and antiviral effects. Pixatimod effectively inhibits SARS-CoV-2 by disrupting the spike protein-ACE2 interaction. Additionally, it blocks various cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These effects have demonstrated significant efficacy in numerous mouse cancer models, including about 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, showing clinical potential when used with gemcitabine, paclitaxel, sorafenib, platinum compounds, and anti-PD-1 antibodies.

Pixatimod (also known as PG-545) is a synthetic modified heparan sulfate mimetic and an agonist of Toll-like receptor 9 (TLR9), showcasing potential immunostimulatory, antitumor, and antiviral properties. It effectively inhibits SARS-CoV-2 by disrupting the interaction between the spike protein and ACE2. Moreover, Pixatimod blocks cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These activities have demonstrated significant efficacy across various murine cancer models, including approximately 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, underscoring its clinical potential, with drugs like gemcitabine, paclitaxel, sorafenib, platinum-based compounds, and an anti-PD-1 antibody.