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Catalog No. T6626   CAS 898044-15-0
Synonyms: PF 3758309, PF-309, PF-03758309, PF3758309

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

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PF-3758309, CAS 898044-15-0
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-03758309 (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.
Targets&IC50 PAK3:99 nM, PAK6:17.1 nM(Ki), PAK4:1.3 nM, PAK4:18.7 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.
Kinase Assay 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).
Cell Research 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.
Animal Research Nude mice with Xenograft tumors were orally fed with PF-3758309(7.5-30 mg/kg BID)dissolved in 0.5% methylcellulose.
Synonyms PF 3758309, PF-309, PF-03758309, PF3758309
Molecular Weight 490.63
Formula C25H30N8OS
CAS No. 898044-15-0


Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 91 mg/mL (185.5 mM)

Ethanol: 91 mg/mL (185.5 mM)

H2O: <1 mg/mL

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

References and Literature

1. Murray BW, et al. Proc Natl Acad Sci U S A, 2010, 107(20), 9446-9451.

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PF-3758309 898044-15-0 凋亡 细胞骨架 Apoptosis PAK proliferation tumor oncogenic PF 3758309 survival PF03758309 PF3758309 inhibit p21 activated kinases signaling PF-309 ATP-competitive Inhibitor PF 03758309 PF-03758309 growth inhibitor