1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

PF-04957325 

Cat. No.: HY-15426 Purity: 98.48% ee.: 100.00%
Handling Instructions

PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC50 values of 0.7 nM for PDE8A and less than 0.3 nM for PDE8B.

For research use only. We do not sell to patients.

PF-04957325 Chemical Structure

PF-04957325 Chemical Structure

CAS No. : 1305115-80-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 370 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC50 values of 0.7 nM for PDE8A and less than 0.3 nM for PDE8B.

IC50 & Target

IC50: 0.7 nM (PDE8A), less than 0.3 nM (PDE8B)[1]

In Vitro

PF-04957325 is over two orders of magnitude less efficient than PICL in suppressing polyclonal Teff cell proliferation, and shows no effect on cytokine gene expression in these cells, despite its robust effect on T cell adhesion[1]. PF-04957325 is a selective PDE8 inhibitor and inhibits breast cancer cell migration[2]. PF-04957325 greatly potentiates steroidogenesis in WT adrenal cells. PF-04957325 shows a reported IC50 of 0.7 nM against PDE8A, 0.2 nM against PDE8B, and > 1.5 μM against all other PDE isoforms[3]. PF-04957325 treatment of WT Leydig cells or MA10 cells increases steroid production but has no effect in PDE8A (-/-)/B(-/-) double-knockout cells, confirming the selectivity of the drug. Moreover, under basal conditions, cotreatment with PF-04957325 plus rolipram, a PDE4-selective inhibitor, synergistically potentiates steroid production[4].

Solvent & Solubility
In Vitro: 

DMSO : 9.9 mg/mL (24.73 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4976 mL 12.4881 mL 24.9763 mL
5 mM 0.4995 mL 2.4976 mL 4.9953 mL
10 mM 0.2498 mL 1.2488 mL 2.4976 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

Breast cancer cells are in a total volume of 0.1 mL of fresh medium containing the test reagents or vehicle (PF-04957325). Following incubation at 37°C for 72 h, 20 μL of a combined solution of MTS (2 mg/mL)/PMS (0.92 mg/mL) (20:1, mixed immediately before use) is added to each well, and the plates incubated for an additional 2 h at 37°C, protected from light, following which the absorbency of the formazan product formed is determined at 492 nm using a microtiter plate reader. All reagents tested are dissolved in DMSO and diluted into the cell culture medium[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

400.38

Formula

C₁₄H₁₅F₃N₈OS

CAS No.

1305115-80-3

SMILES

NC1=C(N=NN2C[[email protected]]3CN(CC4=NC=CS4)CCO3)C2=NC(C(F)(F)F)=N1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PF-04957325
Cat. No.:
HY-15426
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PF-04957325

Cat. No.: HY-15426