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G-5555 hydrochloride
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G-5555 hydrochloride
MCE 站:G-5555 hydrochloride
产品活性:G-5555 hydrochloride是有效,选择性的PAK1抑制剂,Ki值为3.7 nM。
研究领域:Cell Cycle/DNA Damage | Cytoskeleton
作用靶点:PAK
In Vitro: G-5555 shows excellent kinase selectivity and inhibits only eight out of the 235 kinases tested other than PAK1 with inhibition >70%: PAK2, PAK3, KHS1, Lck, MST3, MST4, SIK2, and YSK1. The IC50s of G-5555 against SIK2, PAK2, KHS1, MST4, YSK1, MST3 and Lck are 9, 11, 10, 20, 34, 43, 52 nM, respectively. In general, G-5555 demonstrates high selectivity for the group I PAKs. There is negligible activity for G-5555 against the hERG channel with IC50 more than 10 μM in a patch clamp assay. In an array of 23 breast cancer cell lines, G-5555 has significantly greater growth inhibitory activity in cell lines that are PAK-amplified compared to non-amplified lines.
In Vivo: G-5555 exhibits low blood clearance and an acceptable half-life. Good oral exposure (AUC=30 μM?h) and high oral bioavailability (F=80%) are achieved. In an H292 non-small cell lunger cancer (NSCLC) xenograft study in mice, G-5555 inhibits phosphorylation of the PAK1/2 downstream substrate mitogen-activated protein kinase 1 (MEK1) S298 and, when administered at an oral dose of 25 mg/kg b.i.d., imparts 60% tumor growth inhibition in this model13 and a PAK1 amplified breast cancer xenograft model, MDAMB-175.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Cytoskeleton Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Fingolimod hydrochloride | IPA-3 | 5-Aminosalicylic Acid | FRAX597 | FRAX486 | NVS-PAK1-1 | G-5555 | GNE 2861 | FRAX1036 | LCH-7749944 | Mesalamine impurity P | NVS-PAK1-C
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