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Gemcitabine is an anticancer nucleoside analog that inhibits the growth of HL-60 promyelocytic leukemia cells with an LC50 value of 40 nM.{40344} It inhibits the growth of MX-1 mammary, CX-1, HC-1, GC3, and VRC5 colon, LX-1, Calu-6, and NCI-H460 lung, and HS766T, PaCa-2, PANC-1, and BxPC-3 pancreatic cancer tumors in mouse xenograft models (45-93% inhibition).{40343} Gemcitabine is a prodrug that is metabolized to a diphosphate and triphosphate form in cells. The triphosphate form is incorporated into DNA which induces masked chain termination and cell death.{21021} By specifically inhibiting growth arrest and DNA damage inducible protein 45 a (Gadd45a), a key mediator of active DNA demethylation, gemcitabine, at concentrations ranging from 34 to 134 nM, inhibits repair-mediated DNA demethylation in a methylation-sensitive reporter assay. Gemcitabine also has broad antiretroviral activity, decreasing MuLV cell infectivity, a murine AIDS model, in cell culture (EC50 = ~1.5 nM) and inhibits the progression of murine AIDS in vivo at a dose of 1-2 mg/kg per day.{21022}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 100 mg, 25 mg, 50 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 122111-03-9 |
| Molecular formula | C9H11F2N3O4 • HCl |
| Smiles | OC[C@H]1O[C@@H](N2C=CC(N)=NC2=O)C(F)(F)[C@@H]1O.Cl |
| Molecular weight | 299,7 |
| Custom code | 2933.49 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
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Prostaglandin I synthase (PGIS) catalyzes the isomerization of PGH2 to PGI2. PGI2 (prostacyclin) is a potent vasodilator and inhibitor of...
Amyloid-? (1-8, A2V) is a truncated form of amyloid-? (A?) that contains a valine to alanine substitution at position 2...
Programmed cell death protein 4 (PDCD4) levels are elevated during apoptosis and absent in many cancer samples.{16340,16167} Loss of PDCD4...
This mixture contains primary prostaglandins produced from arachidonic acid and dihomo-?-linolenic acid. Contents: Prostaglandin E1, Prostaglandin E2, Prostaglandin F1?, 6-keto...
Platelet-activating factor (PAF) is an important lipid mediator involved in inflammation. PAF-acetylhydrolase (PAF-AH) is an extracellular phospholipase A2 which hydrolyzes...
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Protein phosphorylation is an important post-translational modification that serves many key functions to regulate a protein’s activity, localization, and protein-protein...
Proprotein convertase subtilisin kexin 9 (PCSK9) is a member of the subtilisin serine protease family with an important role in...
This mixture contains the characteristic metabolites of both PGI2 and TXA2. Contents: Thromboxane B2, 11-dehydro Thromboxane B2, 6-keto Prostaglandin F1?,...
TAF10 is one of many protein factors or coactivators associated with RNA polymerase II activity.{16903} One vial of this peptide...
This mixture contains the primary metabolites of prostaglandins (PGs) D2, E2, and F2?. Contents: 13,14-dihydro-15-keto PGD2, 13,14-dihydro-15-keto PGE2, 11?-PGF2?, 13,14-dihydro-15-keto...
The Cayman COX Inhibitor Pack contains a combination of frequently used cyclooxygenase (COX) inhibitors. Each kit contains aspirin, the archetype...
GST-tag Polyclonal Antibody (FITC) is a probe for the immunochemical detection of GST tags on recombinant proteins. Recombinant proteins are...
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