Powder: -20°C for 3 years | In solvent: -80°C for 1 year
G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 1,395 | 待询 | ||
10 mg | ¥ 2,245 | 待询 | ||
25 mg | ¥ 4,795 | 待询 | ||
50 mg | 待询 | 待询 | ||
100 mg | 待询 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,620 | 待询 |
G-5555 hydrochloride (1648863-90-4 free base) 的其他形式现货产品:
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. |
靶点活性 | PAK2:11 nM (ki), PAK1:3.7 nM (ki) |
体外活性 | 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.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. |
体内活性 | 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.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. |
别名 | G-5555 hydrochloride |
分子量 | 529.42 |
分子式 | C25H26Cl2N6O3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (188.89 mM), Sonication is recommended.
H2O: 16.67 mg/mL (31.49 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 1.8889 mL | 9.4443 mL | 18.8886 mL | 47.2215 mL |
5 mM | 0.3778 mL | 1.8889 mL | 3.7777 mL | 9.4443 mL | |
10 mM | 0.1889 mL | 0.9444 mL | 1.8889 mL | 4.7221 mL | |
20 mM | 0.0944 mL | 0.4722 mL | 0.9444 mL | 2.3611 mL | |
DMSO | 50 mM | 0.0378 mL | 0.1889 mL | 0.3778 mL | 0.9444 mL |
100 mM | 0.0189 mL | 0.0944 mL | 0.1889 mL | 0.4722 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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