VD/VDR- vd-vdr

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Posts by VD/VDR- vd-vdr

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.

 June 21, 2017

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,…

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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

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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

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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…

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IC50s for GSK1904529A in tumor cell lines ranged from 35 nmol/L to >30 umol/L.The tumor histologic types showing the greatest sensitivity to this compound were Ewing¡¯s sarcoma and multiple myeloma, where IC50s in three of five Ewing¡¯s sarcoma cell lines were <100 nmol/L and IC50s in five of eight multiple myeloma cell lines were <200 nmol/L .

prudect name : IC50s for GSK1904529A in tumor cell lines ranged from 35 nmol/L to >30 umol/L.The tumor histologic types showing the greatest sensitivity to this compound were Ewing¡¯s sarcoma…

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GNF-2 is Bcr-abl inhibitor.

prudect name : GNF-2 is Bcr-abl inhibitor.GNF-2 Synonyms: CAS NO: 778270-11-4Molecular Formula: C18H13F3N4O2Molecular Weight: 374.32Purity: 98% minSolubility: In DMSOStorage: −20°C SYN115 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18515569

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GSK690693 is an aminofurazan-derived£¬novel ATP-competitive, low-nanomolar pan-Akt kinase inhibitor. It is selective for the Akt isoforms(inhibits Akt kinases 1, 2, and 3 with IC50 values of 2, 13, and 9 nM respectively)versus the majority of kinases in other families; however, it does inhibit additional members of the AGC kinase family.

prudect name : GSK690693 is an aminofurazan-derived£¬novel ATP-competitive, low-nanomolar pan-Akt kinase inhibitor. It is selective for the Akt isoforms(inhibits Akt kinases 1, 2, and 3 with IC50 values of 2,…

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GSK2636771 is a potent, orally bioavailable, PI3K beta-selective inhibitor, currently in Phase I/II trials.

prudect name : GSK2636771 is a potent, orally bioavailable, PI3K beta-selective inhibitor, currently in Phase I/II trials.GSK2636771 Synonyms: CAS NO: 1372540-25-4Molecular Formula: C22H22F3N3O3Molecular Weight: 433.42Purity: 98% minSolubility: In DMSOStorage: -20°C…

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Gemfibrozil for hyperlipidemia. For serious or type ¢õ ¢ô hyperlipoproteinemia, coronary heart disease risk of large and diet control, weight loss and other treatment ineffective

prudect name : Gemfibrozil for hyperlipidemia. For serious or type ¢õ ¢ô hyperlipoproteinemia, coronary heart disease risk of large and diet control, weight loss and other treatment ineffectiveGemfibrozil Synonyms: CAS…

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GDC-0068 is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GDC-0068 binds to and inhibits the activity of Akt in a non-ATP-competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

prudect name : GDC-0068 is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GDC-0068 binds to and inhibits the…

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