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PF-00562271

Cat. No. M3286
PF-00562271 Structure
Size Price Availability Quantity
5mg USD 210 In stock
10mg USD 360 In stock
50mg USD 945 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PF-00562271 (PF-562271) is a potent ATP-competitive FAK and proline-rich tyrosine kinase (Pyk2) inhibitor with potential antineoplastic and antiangiogenic activities. Focal adhesion kinase (FAK) transduces signaling from integrins and growth factors to modulate tumor cell invasion, proliferation and survival. Focal adhesion kinase (FAK) is a non-receptor protein tyrosine kinase located in the cytoplasm at focal adhesions – sites that link the extracellular matrix to the cytoplasmic cytoskeleton. Not only do FAKs therefore play a pivotal role in cell migration, but they also influence cell survival and are upregulated in a broad spectrum of epithelial cancers. PF-00562271 (PF-562271) may inhibit tumor cell migration, proliferation, and survival. As FAK is a signal transducer for integrins, inhibition of FAK by PF-00562271 (PF-562271) may prevent integrin-mediated activation of several downstream signals including ERK, JNK/MAPK and PI3K/Akt. FAK and PYK2, upregulated in many tumor cell types, are involved in tumor cell invasion, migration and proliferation.

Protocol
Cell Experiment
Cell lines Squamous cell carcinoma (SCC)
Preparation method Plating cells for 48 hours before addition of PF-562271. 3 days later, cells are fixed by addition of ice cold 25% trichloroacetic acid (TCA) solution prior to staining with Sulforhodamine B (SRB) dye solution. Washing the plates with 1% glacial acetic acid, air-dried and resuspended in 10 mM Tris buffer, pH 10.5 before reading absorbance at 540 nm.Using GraphPad Prism 4 software for curve fitting and carrying out generation of IC50 values from six replicates.
Concentrations 0 to 1 μM
Incubation time 72 hours
Animal Experiment
Animal models PC-3M, BT474, BxPc3, LoVo, U87MG, H125 and H460 cells are injected s.c. into the right flank of athymic female mice
Formulation PF-562271 is dissolved in 5% Gelucire.
Dosages ≤100 mg/kg
Administration Administered via p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 665.66
Formula C21H20F3N7O3S.C6H6O3S
CAS Number 939791-38-5
Purity >99%
Solubility DMSO 10 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-00562271 supplier, FAK, inhibitors

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