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PF-00562271

Cat. No. M3286
PF-00562271 Structure
Synonym:

PF562271 besylate; PF 562271 besylate

Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 180  USD180 In stock
50mg USD 450  USD450 In stock
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Quality Control & Documentation
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 (for reference only)
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.
Chemical Information
Molecular Weight 665.66
Formula C21H20F3N7O3S.C6H6O3S
CAS Number 939791-38-5
Solubility (25°C) DMSO 10 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] Yun Liang, et al. CX3CL1 involves in breast cancer metastasizing to the spine via the Src/FAK signaling pathway

[2] Andrea Maddalena, et al. High-Throughput Screening Identifies Kinase Inhibitors That Increase Dual Adeno-Associated Viral Vector Transduction In Vitro and in Mouse Retina

[3] Brian Y Lee, et al. FAK signaling in human cancer as a target for therapeutics

[4] Brian Y Lee, et al. Phosphoproteomic profiling identifies focal adhesion kinase as a mediator of docetaxel resistance in castrate-resistant prostate cancer

[5] Jeffrey R Infante, et al. Safety, pharmacokinetic, and pharmacodynamic phase I dose-escalation trial of PF-00562271, an inhibitor of focal adhesion kinase, in advanced solid tumors

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  Catalog
Abmole Inhibitor Catalog




Keywords: PF-00562271, PF562271 besylate; PF 562271 besylate supplier, FAK, inhibitors, activators


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