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PF8380

Cat. No. M3700
PF8380 Structure
Size Price Availability Quantity
5mg USD 55  USD55 In stock
10mg USD 80  USD80 In stock
50mg USD 320  USD320 In stock
100mg USD 580  USD580 In stock
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Quality Control & Documentation
Biological Activity

Pf-8380 is a potent autotaxin inhibitor with IC50 of 2.8 nM and 101 nM in in vitro enzyme assay and human whole blood cell assay, respectively.

Chemical Information
Molecular Weight 478.33
Formula C22H21Cl2N3O5
CAS Number 1144035-53-9
Solubility (25°C) DMSO 5 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Bhave SR, et al. Front Oncol. Autotaxin Inhibition with PF-8380 Enhances the Radiosensitivity of Human and Murine Glioblastoma Cell Lines.

[2] St-Cœur PD, et al. Arch Pharm (Weinheim). PF-8380 and closely related analogs: synthesis and structure-activity relationship towards autotaxin inhibition and glioma cell viability.

[3] Gierse J. J Pharmacol Exp Ther. A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.

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