PF 3758309 dihydrochloride

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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)

Biological Activity for PF 3758309 dihydrochloride

PF 3758309 dihydrochloride is a potent PAK4 inhibitor (IC50 = 1.3 nM; Kd = 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

External Portal Information for PF 3758309 dihydrochloride 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.

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.

Technical Data for PF 3758309 dihydrochloride

M. Wt 563.55
Formula C25H30N8OS.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 91885498
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 Data for PF 3758309 dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for PF 3758309 dihydrochloride

Certificate of Analysis / Product Datasheet
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References for PF 3758309 dihydrochloride

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

Murray et al (2010) 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. 107 9446 PMID: 20439741

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Citations for PF 3758309 dihydrochloride

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