首页 Cytoskeletal Signaling PAK PF3758309
PF3758309
编号 T6626     别名: PF 3758309, PF-3758309, PF-03758309, PF-309, PF-3758309, PF-309, PF-03758309 PF 3758309
CAS 898044-15-0     分子式 C25H30N8OS     分子量 490.62
靶点: PAK1; PAK3; PAK4; PAK5; PAK6;
PF-03758309 (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.
选择批次  
纯度 98.0%
规格 库存 单价 数量
5 mg 待询 489.00
10 mg 待询 727.00
50 mg 待询 2437.00
100 mg 待询 4147.00
200 mg 待询 6220.00
1 mL * 10 mM (in DMSO) 待询 489.00
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生物活性

产品描述

PF-03758309 (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.

靶点活性

PAK1,13.7nM(Ki)

PAK3,99nM

PAK4,18.7nM(Ki)

PAK5,18.1nM(Ki)

PAK6,17.1nM(Ki)

体外活性

PF-3758309 (Kd = 2.7 nM), an effective inhibitor of PAK4 (Ki=18.7 nM), has ATP competition. PF-3758309 (IC50 = 1.3 nM) inhibits phosphorylation of the PAK4 substrate GEF-H1 in cells. In the tumor cell, PF-3758309(IC50 = 4.7 nM) grows in a linesanchorage-independent manner. In HCT116 cells, PF-3758309 inhibits endogenous pGEF-H1 accumulation. In A549 cells, PF-3758309 effectively inhibits cellular proliferation in IC50 of 20 nM and anchorage-independent growth in IC50 of 27 nM.

体内活性

In the HCT116 tumor model, PF-3758309 act as an antiproliferative inducing apoptosis. In the sensitive model, PF-3758309 (EC50=0.4 nM) blocks the growth of multiple human tumor xenografts.

激酶实验

In phospho-GEF-H1 cellular assay, TR-293-KDG cells are incubated for 3 hours with PF-3758309. TR-293-KDG cells were captured on an anti-HA antibody-coated plate, which is detected with an anti-phospho-S810-GEF-H1 antibody, and quantified with a horseradish peroxidase-goat anti-rabbit antibody conjugate. TR-293-KDG cells are constructed from HEK293 cells, which is transfected with tetracycline-inducible PAK4-kinase domain (amino acids 291-591) and expressed HA-tagged GEFH1ΔDH (amino acids 210-921).

细胞实验

HEK293T, HCT116, and SKOV3 cells are plated on 384-well plates for 24 hours culture. PF-3758309( ~1 μM) is added to the cell culture incubating 72 hours. After drug treatment,cell proliferation and other indicators of metabolism are measured.

细胞系: HEK293T, HCT116, and SKOV3 cells

动物实验

Nude mice with Xenograft tumors were orally fed with PF-3758309(7.5-30 mg/kg BID)dissolved in 0.5% methylcellulose.

动物模型:Xenograft tumors in nude mice

化学信息

分子量

490.62

分子式

C25H30N8OS

CAS

898044-15-0

溶解度

DMSO: 91 mg/mL (185.5 mM)

Ethanol: 91 mg/mL (185.5 mM)

Water: <1 mg/mL

( < 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 2.038 ml 10.191 ml 20.382 ml
5 mM 0.408 ml 2.038 ml 4.076 ml
10 mM 0.204 ml 1.019 ml 2.038 ml
50 mM 0.041 ml 0.204 ml 0.408 ml
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