首页 Cytoskeletal Signaling PAK G-5555
G-5555
编号 T11342L    
CAS 1648863-90-4     分子式 C25H25ClN6O3     分子量 492.96
靶点: PAK1; PAK2;
G-5555 is a potent inhibitor of p21-activated kinase 1 (PAK1) (Kis: 3.7 nM and 11 nM for PAK1 and PAK2, respectively).
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 8110.00
100 mg 待询 14485.00
200 mg 待询 待询
500 mg 待询 待询
1 mL * 10 mM (in DMSO) 待询 1510.00
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生物活性

产品描述

G-5555 is a potent inhibitor of p21-activated kinase 1 (PAK1) (Kis: 3.7 nM and 11 nM for PAK1 and PAK2, respectively).

靶点活性

PAK1,3.7 nM (ki)

PAK2,11 nM (ki)

体外活性

G-5555 shows high selectivity for the group I PAKs and it also 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. There is a negligible activity for G-5555 against the hERG channel in a patch-clamp assay (IC50 >10 μM) [1]. G-5555 potently inhibits PAK2 (Ki: 11 nM). G-5555 has obviously greater growth inhibitory activity in cell lines that are PAK-amplified compared to non-amplified lines, in an array of 23 breast cancer cell lines [2].

体内活性

G-5555 has low blood clearance and an acceptable half-life. Good oral exposure (AUC = 30 μM•h) and high oral bioavailability (F = 80%) are achieved [1]. G-5555 inhibits phosphorylation of the PAK1/2 downstream substrate mitogen-activated protein kinase 1 (MEK1) S298, in an H292 non-small cell lunger cancer (NSCLC) xenograft study in mice. 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 [2].

化学信息

分子量

492.96

分子式

C25H25ClN6O3

CAS

1648863-90-4

溶解度

DMSO: 27 mg/mL (54.77 mM)

( < 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 2.029 ml 10.143 ml 20.286 ml
5 mM 0.406 ml 2.029 ml 4.057 ml
10 mM 0.203 ml 1.014 ml 2.029 ml
50 mM 0.041 ml 0.203 ml 0.406 ml
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