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AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, AZD3759 binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. This prevents EGFR-mediated signaling, and may lead to both induction of cell death and inhibition of tumor growth in EGFR-overexpressing cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. Check for active clinical trials using this agent. (NCI Thesaurus)

June 21, 2017

prudect name : AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, AZD3759 binds to and inhibits the activity…

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AZD8835 is a selective, oral inhibitor of PI3K isoforms ¦Á and ¦Ä with the following activity in enzymatic assays: PI3K ¦Á ¨C IC50 = 6nM (equipotent vs wt and E545K / H1047R mutants); PI3K ¦Ä ¨C IC50 = 6nM; PI3K ¦Ã ¨C IC50 = 90nM; PI3K ¦Â ¨C IC50 = 431nM. Inhibition of signalling in cells (pAKT endpoint): PI3K ¦Á ¨C IC50= 57nM; PI3K ¦Ä ¨C IC50= 49nM; PI3K ¦Â ¨C IC50= 3.6¦ÌM; PI3K ¦Ã- IC50= 532nM

prudect name : AZD8835 is a selective, oral inhibitor of PI3K isoforms ¦Á and ¦Ä with the following activity in enzymatic assays: PI3K ¦Á ¨C IC50 = 6nM (equipotent vs…

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Akt Inhibitor VIII is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity (IC50 = 58 nM, 210 nM, and 2.12 _mu_M; respectively).

prudect name : Akt Inhibitor VIII is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity (IC50 = 58…

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prudect name : AZ-7371Synonyms: CAS NO: 1494675-86-3Molecular Formula: Molecular Weight: Purity: 98% minSolubility: DMSOStorage: -20¡æ

prudect name : AZ-7371 Synonyms: CAS NO: 1494675-86-3Molecular Formula: Molecular Weight: Purity: 98% minSolubility: DMSOStorage: -20¡æ 850664-21-0 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18500569

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AZD6482 is a PI3K_beta_ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3K_beta_ than PI3K_delta_, PI3K_alpha_ and PI3K_gamma

prudect name : AZD6482 is a PI3K_beta_ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3K_beta_ than PI3K_delta_, PI3K_alpha_ and PI3K_gammaAZD 6482 Synonyms: CAS NO:…

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Apoptosis activator; promotes the cytochrome c-dependent oligomerization of Apaf-1 into the mature apoptosome. Increases procaspase-9 processing and subsequent caspase-3 activation. Induces apoptosis in tumor cells (IC50 = 4 – 9 ¦ÌM for leukemia cells) with weak or no effect on normal cell lines or those defective/deficient in Apaf-1, caspase-9 or caspase-3 activity (IC50 > 40 ¦ÌM).

prudect name : Apoptosis activator; promotes the cytochrome c-dependent oligomerization of Apaf-1 into the mature apoptosome. Increases procaspase-9 processing and subsequent caspase-3 activation. Induces apoptosis in tumor cells (IC50 =…

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AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator and antagonist. AZD9496 can induce ER¦Á degradation in breast cancer cell lines at picomolar concentrations. AZD9496 is curently under clinical trials. AZD9496 may be useful for the treatment of ER+ breast cancer.

prudect name : AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator and antagonist. AZD9496 can induce ER¦Á degradation in breast cancer cell lines at picomolar concentrations. AZD9496…

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AM580(Am-580; Ro 40-6055; NSC608001; CD336) is a stable retinobenzoic derivative originally synthesized as a RAR¦Á agonist. IC50 value: Target: RAR¦Á agonist in vitro: AM580 is a powerful inducer of granulocytic maturation in NB4, an APL-derived cell line, and in freshly isolated APL blasts. After treatment of APL cells with AM580 either alone or in combination with granulocyte colony-stimulating factor (G-CSF), the compound induces granulocytic maturation, as assessed by determination of the levels of leukocyte alkaline phosphatase, CD11b, CD33, and G-CSF receptor mRNA, at concentrations that are 10- to 100-fold lower than those of ATRA necessary to produce similar effects . in vivo: A dose of 0.3mg/kg/day of Am580, was tested by treating 10 FVB mice for 4 months; no overt toxicity was found in liver, lungs, kidney, and spleen . Treatment of MMTV-Myc mice with the RAR¦Á-selective agonist Am580 led to significant inhibition of mammary tumor growth (~90%, P<0.001), lung metastasis (P<0.01) and extended tumor latency in 63% of mice. Immunocytochemical analysis showed that in these mice, RAR¦Á responsive genes such as Cyp26A1, E-cadherin, cellular retinol-binding protein 1 (CRBP1) and p27, were up-regulated

prudect name : AM580(Am-580; Ro 40-6055; NSC608001; CD336) is a stable retinobenzoic derivative originally synthesized as a RAR¦Á agonist. IC50 value: Target: RAR¦Á agonist in vitro: AM580 is a powerful…

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Chemical Name: N-[[4-(1,4,8,11-Tetraazacyclotetradec-1-ylmethyl)phenyl]methyl]-2-pyridinemethanamine hexahydrobromide

prudect name : Chemical Name: N-[[4-(1,4,8,11-Tetraazacyclotetradec-1-ylmethyl)phenyl]methyl]-2-pyridinemethanamine hexahydrobromideAMD 3465 hexahydrobromide Synonyms: CAS NO: 185991-07-5Molecular Formula: C24H38N6.6HBrMolecular Weight: 896.07Purity: 98% minSolubility: In DMSOStorage: −20°C 32222-06-3 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18500378

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AZD2014 is a close analogue of AZD8055 and a selective inhibitor of mTOR kinase. AZD2014 has greater inhibitory activity against mTORC1 compared to rapamycin: AZD2014 decreases p4EBP1 Thr37/46, inhibits the translation initiation complex and decreases overall protein synthesis while rapamycin has no effect. AZD2014 also inhibits the mTORC2 biomarkers pAKTSer473 and pNDRG1Thr346. AZD2014 has broad antiproliferative activity across multiple tumour cell lines. In particular, AZD2014 induces growth inhibition and cell death in breast cancer cell lines, including ER+ cell lines with acquired resistance to hormone therapy.

prudect name : AZD2014 is a close analogue of AZD8055 and a selective inhibitor of mTOR kinase. AZD2014 has greater inhibitory activity against mTORC1 compared to rapamycin: AZD2014 decreases p4EBP1…

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