化合物PF3758309 T6626

Product Introduction
Bioactivity


英文名: PF-3758309

描述: PF-3758309 (PF-03758309) 是一种可口服的、可逆的 ATP 竞争性 PAK4抑制剂。它是一种 PAK4 抑制剂，可抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。

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.

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).

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.

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 91 mg/mL (185.5 mM)
Ethanol : 91 mg/mL (185.5 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: PF-3758309 | proliferation | tumor | oncogenic | survival | PF03758309 | inhibit | p21 activated kinases | signaling | Apoptosis | ATP-competitive | PF 309 | PF 03758309 | Inhibitor | PF3758309 | growth | PF309 | PAK

相关产品: L-Cystathionine | Ziyuglycoside II | Decitabine | Stavudine | Sunitinib Malate | GSK-3β inhibitor 3 | Rhapontin | Pantoprazole sodium | ARS-853 | Pranoprofen

相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Orally Active Compound Library | Bioactive Compound Library

化合物PF3758309 T6626信息由TargetMol中国为您提供，如您想了解更多关于化合物PF3758309 T6626报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途