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产品介绍 Gefitinib is a tyrosine kinase inhibitor. It is a potent inhibitor of EGFR kinase (Ki = 0.40 nM), but much weaker against ErbB-2 kinase (Ki = 870 nM) and ErbB-4 kinase (Ki = 1.1 µM).
询价产品介绍 Potent and selective inhibitor of phosphatidyl-inositol 3-kinase. Active in purified preparations and cytosolic fractions(IC50 = 5nM) and is highly cell permeable. Covalently binds to PI 3-kinase and is selective, inhibiting other kinases such as PI 4-kinase and myosin light chain kinase at concentrations 100-fold higher than that required for inhibition of PI 3-kinase.
询价产品介绍 Dihydrochloride form of HA-1077. Inhibits a number of kinases, including ROCK I (IC50 = 10.7 µM), ROCK II (IC50 = 1.9 µM), MAPK1 (IC50 = 5 µM), and PKCRK2 (IC50 = 4 µM). Weaker inhibitor of PKC (IC50 = 425 µM) and MLCK (IC50 = 95 µM) .
询价产品介绍 Monohydrochloride form of HA-1077. Inhibits a number of kinases, including ROCK I (IC50 = 10.7 µM), ROCK II (IC50 = 1.9 µM), MAPK1 (IC50 = 5 µM), and PKCRK2 (IC50 = 4 µM). Weaker inhibitor of PKC (IC50 = 425 µM) and MLCK (IC50 = 95 µM) .
询价产品介绍 Potent (Ki, 0.6 nM), specific and reversible proteasome inhibitor; no significant inhibitory activity against other enzymes or receptors. Bortezomib inhibits cell proliferation of H460 cells (human non-small cell lung cancer cell lines) with an IC50 of 0.1 µM and has been associated with suppresion of prostate cancer cell lines with an IC90 of 10 nM.
询价产品介绍 17-AAG binds specifically to heat shock protein Hsp90 in a manner similar to geldanamycin, but the binding is weaker. Inhibits Akt activation and HER2 expression in tumor cells. Exhibits 100-fold higher binding affinity for tumor-cell-derived hsp90 over that derived from normal cells. Inhibits angiogenesis.
询价背景介绍 Heat shock protein 90 (HSP90) is a molecular chaperone essential for the stability of key regulators of cell growth and survival. HSP90 is involved in protein folding and functions as a chaperone for numerous client proteins, many of which are important in cancer pathogenesis. Hsp90 enables cancer cell survival by maintaining the function of their mutated client proteins including the KIT and PDGFRA proteins. AUY922 inhibits Hsp90, resulting in proteasomal degradation of oncogenic client proteins, inhibition of cell proliferation, and elevation of HSP72 levels in a wide range of human tumor cell lines. 产品介绍 NVP-AUY922 potently inhibits HSP90 with IC50 values of 7.8 nM and 21 nM, and Ki values of 9 nM and 8.2 nM for HSP90α and HSP90β, respectively. NVP-AUY922 shows a very high binding affinity to HSP90β with a Kd of 1.7 nM. NVP-AUY922 inhibits the proliferation of human tumor cells in vitro with GI50 values of approximately 2 to 40 nM, inducing G1-G2 arrest and apoptosis. Human endothelial cells are very sensitive to NVP-AUY922 with GI50s of 2.5-3.9 nM. NVP-AUY922 also exhibits potent antitumor efficacy in human tumor xenografts including BT474 breast, A2780 ovarian, U87MG glioblastoma, PC3 prostate, and WM266.4 melanoma.
询价产品介绍 Temsirolimus, a rapamycin (sirolimus) derivative, also known as CCI-779, is an mTOR inhibitor with anti-cancer activity. Temsirolimus down-regulated the mTOR signaling intermediate phospho-S6 in xenografted human ALL. Temsirolimus has been shown to reverse cisplatin resistance in small cell lung cancer cell lines selected for cisplatin resistance and in cell lines derived from patients who failed cisplatin therapy.
询价产品介绍 Novel, potent and selective JNK-1,-2, and -3 inhibitor (Ki = 0.19 µM). SP600125 is an ATP-competitive reversible inhibitor with >20-fold selectivity vs. a range of kinases and enzymes tested. In cells, SP600125 caused a dose-dependent inhibition of the phosphorylation of c-Jun, the expression of inflammatory genes IL-2, COX-2, TNF-α, IFN-γ, and blocked the activation and differentiation of primary human CD4 cell cultures.
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