VD/VDR-vd-vdr.com

S1RA(E-52862) is a potent and selective sigma-1 receptor(¦Ò1R, Ki=17 nM) antagonist, showed good selectivity against ¦Ò2R (Ki > 1000 nM).

June 21, 2017

prudect name : S1RA(E-52862) is a potent and selective sigma-1 receptor(¦Ò1R, Ki=17 nM) antagonist, showed good selectivity against ¦Ò2R (Ki > 1000 nM).S1RA(E-52862) Synonyms: CAS NO: 878141-96-9Molecular Formula: C20H23N3O2Molecular Weight:…

📌

0💬 read more

Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.

prudect name : Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in…

📌

0💬 read more

Saracatinib is highly selective for Src and Abl kinases against a large range of tyrosine and serine-threonine kinases (VEGFR2, FGFR, c-Kit, Aur-3 etc. >5 µM). Saracatinib exerts its activity through ATP competitive and reversible inhibition of the target enzyme. [1]Saracatinib potently inhibited the in vitro proliferation of Src3T3 mouse fibroblasts and demonstrated variable antiproliferative activity in a range of human cancer cell lines containing endogenous Src. Sub micromolar growth inhibition of five of the human cancer cell lines tested with Saracatinib(tumor types: colon, prostate, lung, and leukemia) was observed with IC50 values of 0.2¨C0.7 µM. In 3-day MTS cell proliferation assays, AZD0530 inhibited in vitro proliferation of the Bcr¨CAbl-driven human leukemia cell line K562 with an IC50 of 0.22 µM.In a head-to-head assay measuring EGFR phosphorylation in KB cells, Saracatinib exhibited an IC50 of 1.25 mM compared with 11 nM for gefitinib.

prudect name : Saracatinib is highly selective for Src and Abl kinases against a large range of tyrosine and serine-threonine kinases (VEGFR2, FGFR, c-Kit, Aur-3 etc. >5 µM). Saracatinib exerts…

📌

0💬 read more

Sunitinib (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 µM for Flk-1 and PDGFR, respectively. In RS4;11 cells (FLT3-WT), addition of FL was necessary to stimulate FLT3 phosphorylation, and treatment with SU11248 inhibited FLT3-WT phosphorylation in a dose-dependent manner with a 50% inhibitory concentration of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, it is noteworthy that both high and low molecular weight forms of FLT3 are phosphorylated in the absence of FLT3 ligand (FL), consistent with expression of FLT3-ITD. Sunitinib Malate (Sutent, SU11248) inhibited FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM following a 2-hour treatment. Evaluating the ability of Sunitinib (Sutent) to inhibit ligand-dependent receptor phosphorylation in cells, the effect of sunitinib (Sutent) on ligand-dependent proliferation of cells was examined. Sunitinib (Sutent) inhibited VEGF- and FGF-induced proliferation of HUVECs with IC50 of 0.04 and 0.7 µM, respectively. Sunitinib (Sutent) also inhibited PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFR¦Á or PDGFR¦Â with IC50 of 0.03 and 0.07 µM, respectively.

prudect name : Sunitinib (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 µM for Flk-1 and PDGFR, respectively. In RS4;11 cells…

📌

0💬 read more

Sorafenib tosylate is the first listing of approved drugs targeting multiple targets, but also over the past decade is the only FDA approved drug for the treatment of renal cell carcinoma.

prudect name : Sorafenib tosylate is the first listing of approved drugs targeting multiple targets, but also over the past decade is the only FDA approved drug for the treatment…

📌

0💬 read more

SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 ¦ÌM, respectively.

prudect name : SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 ¦ÌM, respectively.SGI 7079 Synonyms: CAS NO:…

📌

0💬 read more

6-(2,4-Difluorophenoxy)-8-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride

prudect name : 6-(2,4-Difluorophenoxy)-8-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochlorideSY-R1487;R1487 Synonyms: CAS NO: 449808-64-4Molecular Formula: C19H18F2N4O3.HClMolecular Weight: 424.83Purity: 98% minSolubility: In DMSOStorage: -20 oC web site: www.medchemexpress.com

📌

0💬 read more

SGX523 is a novel, ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L and is >1,000-fold selective versus the >200-fold selectivity of other protein kinases tested in biochemical assays. Crystallographic study revealed that SGX523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases, suggesting an explanation for the selectivity. SGX523 inhibited MET-mediated signaling, cell proliferation, and cell migration at nanomolar concentrations but had no effect on signaling dependent on other protein kinases, including the closely related RON, even at micromolar concentrations. SGX523 inhibition of MET in vivo was associated with the dose-dependent inhibition of growth of tumor xenografts derived from human glioblastoma and lung and gastric cancers, confirming the dependence of these tumors on MET catalytic activity. Our results show that SGX523 is the most selective inhibitor of MET catalytic activity described to date and is thus a useful tool to investigate the role of MET kinase in cancer without the confounding effects of promiscuous protein kinase inhibition.

prudect name : SGX523 is a novel, ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L and is >1,000-fold…

📌

0💬 read more

(5Z)-5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione;TCS PIM-1 4a;SMI-4a

prudect name : (5Z)-5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione;TCS PIM-1 4a;SMI-4aSMI-4a Synonyms: CAS NO: 438190-29-5 327033-36-3 Molecular Formula: C11H6F3NO2SMolecular Weight: 273.23Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com

📌

0💬 read more

SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.

prudect name : SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively….

📌

0💬 read more