prudect name : GestodeneSynonyms: CAS NO: 60282-87-3Molecular Formula: C21H26O2Molecular Weight: 310.43Purity: 99%Solubility: Storage: −20°C

June 21, 2017

prudect name : Gestodene Synonyms: CAS NO: 60282-87-3Molecular Formula: C21H26O2Molecular Weight: 310.43Purity: 99%Solubility: Storage: −20°C SP-600125 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18515809

📌
0💬 read more

Dolutegravir (DTG, GSK1349572) is an integrase inhibitor being developed for the treatment of human immunodeficiency virus (HIV)-1 infection by GlaxoSmithKline (GSK) on behalf of Shionogi-ViiV Healthcare LLC. DTG is metabolized primarily by uridine diphosphate glucuronyltransferase (UGT)1A1, with a minor role of cytochrome P450 (CYP)3A, and with renal elimination of unchanged drug being extremely low (< 1% of the dose). Fifty-three percent of the total oral dose is excreted unchanged in the feces but it is unknown if all or part of this is due to unabsorbed drug or some percentage of biliary excretion of the glucuronide conjugate which can be further degraded to form the parent compound in the gut lumen. The current Food and Drug Administration (FDA) draft guidance for renal impairment studies states that a pharmacokinetic (PK) study in patients with renal impairment should be conducted even for those drugs primarily metabolized or secreted in bile, because renal impairment can inhibit some pathways of hepatic and gut drug metabolism and transport.

prudect name : Dolutegravir (DTG, GSK1349572) is an integrase inhibitor being developed for the treatment of human immunodeficiency virus (HIV)-1 infection by GlaxoSmithKline (GSK) on behalf of Shionogi-ViiV Healthcare LLC….

📌
0💬 read more

Gliclazide mainly for adult onset invalid diet alone, and no ketosis tendency of light, medium Diabetes.

prudect name : Gliclazide mainly for adult onset invalid diet alone, and no ketosis tendency of light, medium Diabetes.Gliclazide Synonyms: CAS NO: 21187-98-4Molecular Formula: C15H21N3O3SMolecular Weight: 323.41Purity: 99%Solubility: Storage: −20°C…

📌
0💬 read more

GDC-0941 against p110a IC50=0.003¦ÌM,U87MG IC50=0.95¦ÌM, A2780 IC50=0.14 ¦ÌM, and in vitro metabolic stability in mouse and human is 91.96%. The inhibitions of U87MG , PC3, MDA-MB-361 cancer cell proliferation are (IC50) 0.95, 0.28, 0.72 ¦ÌM, respectively. ——————————————————————————–

prudect name : GDC-0941 against p110a IC50=0.003¦ÌM,U87MG IC50=0.95¦ÌM, A2780 IC50=0.14 ¦ÌM, and in vitro metabolic stability in mouse and human is 91.96%. The inhibitions of U87MG , PC3, MDA-MB-361 cancer…

📌
0💬 read more

GSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor ¦Á production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC50 (compared with IC50 values of 5, 22, and 389 nM for roflumilast, tofimilast, and cilomilast, respectively) and by LPS-stimulated whole blood with 126 pM IC50. GSK256066 also inhibited LPS-induced increases in exhaled nitric oxide (ED50=35 µg/kg). In addition, GSK256066 prevented pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 ¦Ìg/kg). In ferrets, inhaled GSK256066 inhibited LPS-induced pulmonary neutrophilia (ED50=18 ¦Ìg/kg) and no emetic episodes were observed

prudect name : GSK256066 is an exceptionally high affinity and selective PDE4 inhibitor with an IC50 of 3.2 pM for PDE4B. GSK256066 suppressed tumor necrosis factor ¦Á production by lipopolysaccharide…

📌
0💬 read more

GSK2126458 is a highly potent PI3K and mTOR inhibitor with an app Ki of 19 pM for PI3K. In vivo, GSK2126458 showed anti-tumor activity in both pharmacodynamic and tumor growth efficacy models. In cell, in good agreement with the inhibition of potent PI3K. GSK2126458 reduced the phosphorylated AKT, p70S6K contents in a dose and time dependent way, as well as the prevention of PRAS40 and ERK. The IC50 of GSK2126458 is 2 nM for pAKT in the HCC1954 breast carcinoma cell line. In various human tumor cells, GSK2126458 had a width of inhibitory activity for potent cell growth and induced cell death. Notably, GSK2126458 acted mainly by not induction of apoptosis but cell cycle arrest, particularly in G1-phase.

prudect name : GSK2126458 is a highly potent PI3K and mTOR inhibitor with an app Ki of 19 pM for PI3K. In vivo, GSK2126458 showed anti-tumor activity in both pharmacodynamic…

📌
0💬 read more

Gefitinib (Iressa) is a novel potent EGFR tyrosine kinase and Akt phosphorylations inhibitor with IC50 of 37, 26 and 57 nM for Tyr1173, Tyr1173 and Tyr992 in, respectively, the low and high EGFR expressing cell lines. Immunoblot analysis of whole cell lysates revealed that in general gefitinib effectively inhibited all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines. However, the phosphorylation sites Tyr1173 and Tyr992 were less sensitive requiring higher concentrations of gefitinib for inhibition. As was the case for ERK, gefitinib fails to effectively inhibit AKT phosphorylation in the high-EGFR- expressing cell line indicating that EGFR is not the major activator of AKT in this cell line. The low IC50 (7 nM), however show that the weak induction of AKT phosphorylation by EGFR in this cell line is efficiently blocked by gefitinib. Gefitinib inhibits AKT phosphorylations, with IC50 values of 220 and 263 nM, in the low-EGFR- and ¨CEGFRvIII-expressing cell lines, respectively.

prudect name : Gefitinib (Iressa) is a novel potent EGFR tyrosine kinase and Akt phosphorylations inhibitor with IC50 of 37, 26 and 57 nM for Tyr1173, Tyr1173 and Tyr992 in,…

📌
0💬 read more

prudect name : GW 843682XSynonyms: CAS NO: 660868-91-7Molecular Formula: C22H18F3N3O4SMolecular Weight: 477.46Purity: 98% minSolubility: In

prudect name : GW 843682X Synonyms: CAS NO: 660868-91-7Molecular Formula: C22H18F3N3O4SMolecular Weight: 477.46Purity: 98% minSolubility: In DMSOStorage: −20°C WZ-4003 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18515594

📌
0💬 read more

prudect name : GestrinoneSynonyms: CAS NO: 16320-04-0Molecular Formula: C21H24O2Molecular Weight: 308.42Purity: 98% minSolubility: Storage: −20°C

prudect name : Gestrinone Synonyms: CAS NO: 16320-04-0Molecular Formula: C21H24O2Molecular Weight: 308.42Purity: 98% minSolubility: Storage: −20°C SB525334 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18515590

📌
0💬 read more

Ganetespib (STA-9090) is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor STA-9090 binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogenic client proteins, the inhibition of cell proliferation and the elevation of heat shock protein 72 (Hsp72); it may inhibit the activity of multiple kinases, such as c-Kit, EGFR, and Bcr-Abl, which as client proteins depend on functional HsP90 for maintenance. Hsp90, a 90 kDa molecular chaperone upregulated in a variety of tumor cells, plays a key role in the conformational maturation, stability and function of “client” proteins within the cell, many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition.

prudect name : Ganetespib (STA-9090) is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor STA-9090 binds to and inhibits Hsp90, resulting in…

📌
0💬 read more
« Previous
1 … 693 694 695 696 697 … 825
Next »