PF 3758309 dihydrochloride

Name: PF 3758309 dihydrochloride
Brand: Tocris Bioscience
SKU: 6005

Tocris Bioscience, part of Bio-Techne | Catalog # 6005

COA / SDS

Potent PAK4 inhibitor; orally available

Key Product Details

Description:	Potent PAK4 inhibitor; orally available
Chemical Name:	N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	563.55

View Full Technical Details for PF 3758309 dihydrochloride

Technical Data
Citations

Biological Activity for PF 3758309 dihydrochloride

PF 3758309 dihydrochloride is a potent PAK4 inhibitor (IC₅₀ = 1.3 nM; K_d = 2.7 nM). Inhibits proliferation and anchorage-independent growth of a panel of tumor cell lines in vitro. Suppresses growth of human HCT116 and A549 tumor cell xenografts in mice. Orally available.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc

Compound Libraries for PF 3758309 dihydrochloride

PF 3758309 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 3758309 is reviewed on the Chemical Probes website.

Technical Data for PF 3758309 dihydrochloride

M. Wt	563.55
Formula	C₂₅H₃₀N₈OS.2HCl
Storage	Store at -20°C
Purity	≥98% (HPLC)
PubChem ID	91885498
InChi Key	BTVSNRMSUYBDRT-JQDLGSOUSA-N
Smiles	CN(C[C@H](C1=CC=CC=C1)NC(N2CC3=C(C2(C)C)NN=C3NC4=C5SC=CC5=NC(C)=N4)=O)C.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PF 3758309 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	56.35	100
	DMSO	56.35	100

Preparing Stock Solutions for PF 3758309 dihydrochloride

The following data is based on the product molecular weight 563.55.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.77 mL	8.87 mL	17.74 mL
5 mM	0.35 mL	1.77 mL	3.55 mL
10 mM	0.18 mL	0.89 mL	1.77 mL
50 mM	0.04 mL	0.18 mL	0.35 mL

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Reconstitution Calculator

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References for PF 3758309 dihydrochloride

References are publications that support the biological activity of the product.

Murray Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc.Natl.Acad.Sci.U.S.A. 2010 PMID: 20439741