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PF-3758309

Catalog No. T6626 CAS 898044-15-0

Synonyms: PF-309, PF-03758309, PF 3758309

PF-3758309 (PF-03758309) (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PF-3758309, CAS 898044-15-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 55.00
10 mg	In stock	$ 79.00
25 mg	In stock	$ 145.00
50 mg	In stock	$ 237.00
1 mL * 10 mM (in DMSO)	In stock	$ 59.00

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Purity: 99.37%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PF-3758309 (PF-03758309) (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.
Targets&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.
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-309, PF-03758309, PF 3758309
Molecular Weight	490.62
Formula	C25H30N8OS
CAS No.	898044-15-0

Storage

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

Solubility Information

DMSO: 91 mg/mL (185.5 mM)

Ethanol: 91 mg/mL (185.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Active Compound Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compound Library Anti-Cancer Compound Library Clinical Compound Library Apoptosis Compound Library

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Keywords

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

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