MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 942918-07-2
MCE 国际站:GSK-1070916
产品活性:GSK-1070916是有效,选择性,ATP竞争型的极光激酶B/C (aurora B/C) 抑制剂,Ki 值分别为0.38和1.5 nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics | Apoptosis
作用靶点:Aurora Kinase | Apoptosis
In Vitro: GSK-1070916 potently inhibits Aurora B/INCENP and Aurora C/INCENP kinases with Kis of 0.38±0.29 and 1.45±0.35 nM, respectively, but is less potent against Aurora A/ TPX2 with a Ki of 492±61 nM. GSK-1070916 also inhibits FLT1, TIE2, SIK, FLT4, and FGFR1 with IC50 values of 42, 59, 70, 74, and 78 nM, respectively. Treatment of A549 human lung cancer cells with GSK-1070916 results in a potent antiproliferative effect (EC50=7 nM). GSK-1070916 inhibits a panel of tumor cell lines and is shown o inhibits the phosphorylation of HH3- S10 in all cell lines with average EC50 values ranging from 8 to 118 nM.
In Vivo: In nude mice implanted with human colon tumor (HCT116) xenografts, a single dose of GSK-1070916 administered i.p. inhibits HH3-S10 phosphorylation in a dose-dependent manner. Repeated i.p. administration of GSK-1070916 produces complete or partial antitumor activity in 4 of 8 tumor types [lung, A549; colon, HCT116; acute myelogenous leukemia (AML), HL60; and chronic myelogenous leukemia, K562], stable disease in 3 of 8 (colon, Colo205; lung, H460; and breast, MCF-7), and tumor growth delay in 1 of 8 tumor types (colon, SW620). Daily administration of GSK-1070916 is generally well-tolerated.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Anti-Lung Cancer Compound Library | Anti-Blood Cancer Compound Library | Targeted Diversity Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | Cell Death Library | Serine/Threonine Kinase Inhibitor Library | MG-132 | Doxorubicin hydrochloride | Bafilomycin A1 | LY294002 | Tamoxifen | Paclitaxel | Y-27632 | Acetylcysteine | Angiotensin II human | 2-Deoxy-D-glucose | Staurosporine | SB-431542 | Actinomycin D | Deferoxamine mesylate | Bortezomib | 5-Fluorouracil | Trametinib | Sorafenib | Oxaliplatin | Gemcitabine | Temozolomide | Rotenone | Mdivi-1 | Elesclomol | Ruxolitinib | Decitabine | SP600125 | MK-2206 dihydrochloride | Etoposide | Monomethyl auristatin E
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Dye Reagents | PROTAC | Isotope-Labeled Compounds