Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-3758309 (PF-03758309) (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
5 mg | 在庫あり | ¥ 13,000 | |||
10 mg | 在庫あり | ¥ 18,500 | |||
25 mg | 在庫あり | ¥ 33,500 | |||
50 mg | 在庫あり | ¥ 54,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 13,500 |
説明 | PF-3758309 (PF-03758309) (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition. |
ターゲット&IC50 | PAK3:99 nM, PAK4:1.3 nM, PAK4:18.7 nM(Ki), PAK6:17.1 nM(Ki), PAK5:18.1 nM(Ki) |
In vitro | 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. |
In vivo | 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. |
キナーゼ試験 | 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). |
細胞研究 | 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. |
動物実験 | Nude mice with Xenograft tumors were orally fed with PF-3758309(7.5-30 mg/kg BID)dissolved in 0.5% methylcellulose. |
別名 | PF-309, PF-03758309, PF 3758309 |
分子量 | 490.62 |
分子式 | C25H30N8OS |
CAS No. | 898044-15-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 91 mg/mL (185.5 mM)
Ethanol: 91 mg/mL (185.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. 詳細
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PF-3758309 898044-15-0 Apoptosis Cytoskeletal Signaling PAK PF-309 proliferation tumor oncogenic PF-03758309 PF 3758309 survival PF03758309 inhibit p21 activated kinases signaling ATP-competitive PF 309 PF 03758309 Inhibitor PF3758309 growth PF309 inhibitor