货号	规格	价格	上海	北京	珠海	重庆	武汉
V47561-5mg	≥98%	￥1080.00 V47561-5mg ￥1080.00 3-5天	0 货期：3-5天	-	-	-	-
V47561-10mg	≥98%	￥1580.00 V47561-10mg ￥1580.00 3-5天	0 货期：3-5天	-	-	-	-
V47561-25mg	≥98%	￥3580.00 V47561-25mg ￥3580.00 3-5天	0 货期：3-5天	-	-	-	-
V47561-50mg	≥98%	￥5750.00 V47561-50mg ￥5750.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.

靶点：

PAK1:3.7 nM (Ki);PAK2:11 nM (Ki)

体外研究：

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.

体内研究：

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[1]. 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[2].

参考文献：

1. Ndubaku CO, et al. Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety. ACS Med Chem Lett. 2015 Oct 31;6(12):1241-6.
2. Rudolph J, et al. Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window. J Med Chem. 2016 Jun 9;59(11):5520-41.

保存条件：

2-8°C, 干燥

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.889 ml	9.444 ml	18.889 ml
5 mM	0.378 ml	1.889 ml	3.778 ml
10 mM	0.189 ml	0.944 ml	1.889 ml
50 mM	0.038 ml	0.189 ml	0.378 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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