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GSK-1070916
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GSK-1070916
CAS No. : 942918-07-2
MCE 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 | MG-132 | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Paclitaxel | Y-27632 dihydrochloride | Acetylcysteine | Angiotensin II human | SP600125 | 5-Fluorouracil | Staurosporine | Bortezomib | Tamoxifen | 2-Deoxy-D-glucose | Gemcitabine | Verteporfin | Decitabine | Actinomycin D | Temozolomide | BAY 11-7082 | Etoposide | Mitomycin C | CCCP | DAPT | Rote | Etomoxir | Stattic | Docetaxel | Fulvestrant
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热门标签:GSK-1070916A