PF 3758309 dihydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 6005 - PF 3758309 dihydrochloride | C25H30N8OS.2HCl
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)
Datasheet
Citations
Literature

Biological Activity

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

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 563.55. Batch specific molecular weights may vary from batch to batch due to solvent 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for PF 3758309 dihydrochloride, please let us know.

View Related Products by Target

View Related Products by Product Action

View all P21-activated Kinases Inhibitors

Keywords: PF3758309 dihydrochloride Potent PAK4 inhibitors inhibits orally available 89044_15_0 chemical probes P21-activated Kinases

Citations for PF 3758309 dihydrochloride

Citations are publications that use Tocris products.

Currently there are no citations for PF 3758309 dihydrochloride. Do you know of a great paper that uses PF 3758309 dihydrochloride from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for PF 3758309 dihydrochloride

Protocols

TODO: Add Protocols