首页 Cytoskeletal Signaling PAK G-5555 hydrochloride
G-5555 hydrochloride
编号 T11342    
CAS T11342     分子式 C25H26Cl2N6O3     分子量 529.42
靶点: PAK1; PAK2;
G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
选择批次  
纯度 98.00%
规格 库存 单价 数量
5 mg 待询 1395.00
10 mg 待询 2245.00
25 mg 待询 4795.00
50 mg 待询 待询
100 mg 待询 待询
1 mL * 10 mM (in DMSO) 待询 1620.00
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生物活性

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

PAK1,3.7 nM (ki)

PAK2,11 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.

化学信息

分子量

529.42

分子式

C25H26Cl2N6O3

CAS

T11342

溶解度

DMSO: 100 mg/mL (188.89 mM), Need ultrasonic

H2O: 16.67 mg/mL (31.49 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
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
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