PF-3758309( —— )

Catalog No. M19239 CAS No. 898044-15-0

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PF-3758309
Note

Research use only, not for human use.
Brief Description

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

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

PF-3758309 has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC50=190 nM; PAK3, IC50=99 nM). In cells, PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50=4.7 nM). PF-3758309 also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC50=20 nM) and anchorage-independent growth (IC50=27 nM) of A549 cells.
In Vivo

PF-3758309 (7.5-30 mg/kg; p.o.; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models. Animal Model:Female nu/nu, CRL breed 6–8 weeks old mice (bearing HCT116 and A549 tumors)Dosage:7.5-30 mg/kg Administration:Oral administration; twice daily for 9-18 daysResult:Significant tumor growth inhibition (TGI) in HCT116 and A549 models.
Synonyms

——
Pathway

Membrane Transporter/Ion Channel
Target

NMDAR
Recptor

PAK1| PAK3| PAK4| PAK5| PAK6
Research Area

Cancer
Indication

——

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

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