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PF-562271 HCl FAK inhibitor

Name: PF-562271 HCl
Brand: Selleck Chemicals
SKU: S7357
Availability: InStock
Rating: 5 (34 reviews)

Cat.No.S7357

PF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.

Chemical Structure

Molecular Weight: 543.95

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Quality Control

Batch: Purity: 99.85%

99.85

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2
Other FAK Inhibitors	Defactinib (VS-6063) PF-562271 (VS-6062) PF-573228 VS-4718 (PND-1186) PF-562271 Besylate TAE226 (NVP-TAE226) GSK2256098 PF-431396 Y15 Ifebemtinib (IN10018, BI-853520)

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (183.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (9.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.4mg/ml (0.74mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	543.95	Formula	C₂₁H₂₁ClF₃N₇O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	939791-41-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN(C1=C(C=CC=N1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)C4)S(=O)(=O)C.Cl

Mechanism of Action

Features	Dual FAK/Pyk2 inhibitor that has been tested in Phase I clinical trials for treatment of pancreatic, head and neck, and prostate cancers.
Targets/IC₅₀/Ki	FAK 1.5 nM PYK2 13 nM CDK2/CyclinE 30 nM CDK3/CyclinE 47 nM CDK1/CyclinB 58 nM CDK7/CyclinH/MAT1 97 nM FLT3 97 nM GSK-3α 101 nM CDK5/p35 120 nM GSK-3β 133 nM Aurora A 145 nM
In vitro	PF-562271 binds in the ATP-binding cleft of FAK, forming two of the three “canonical” H-bonds between the inhibitor and main-chain atoms in the kinase hinge region. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. PF-562271 (3.3 μM) results in G1 arrest of PC3-M cells. PF-562271 (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. PF-262271 potently blocks blood vessel sprouting without detectable changes in vascular leakage. PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels.
In vivo	PF-562271 (< 33 mg/kg p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in U87MG-bearing mice. PF-562271 (50 mg/kg p.o. bid) results in 86% tumor growth inhibition in BxPc3 xenografts mice and 45% tumor growth inhibition in PC3-M xenografts mice. PF-562271 (25 mg/kg, bid) results in 2-fold greater apoptosis in treated tumors in mice bearing H125 lung xenografts. PF-562271 (33 mg/kg, p.o.) inhibits extensive movement of the tumor cells over 24 hours in mice. PF-562271 (33 mg/kg, p.o.) results in altered E-cadherin dynamics in mice, which correlates with reduced E-cadherin–dependent collective cell movement. PF-562271 (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. PF-562,271 (5 mg/kg, oral) results in significant and similar increases in osteocalcin and cancellous bone parameters and a decrease in tumor growth and signs of bone healing in rats implanted with MDA-MB-231 cells in the tibia.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18339875/ [2] https://pubmed.ncbi.nlm.nih.gov/18677107/ [3] https://pubmed.ncbi.nlm.nih.gov/21045155/ [4] https://pubmed.ncbi.nlm.nih.gov/20495381/ [5] https://pubmed.ncbi.nlm.nih.gov/18348298/

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