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PF-562271 besylate

An ATP-competitive, reversible inhibitor of FAK
Catalog #: B1253
SKU-Size Size Price Qty
B1253-5 5 mg
$135.00
B1253-25 25 mg
$535.00
More Sizes Get Quote

Product Details

Alternate Name N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl-methanesulfonamide, monobenzenesulfonate
Appearance Off-white solid
CAS # 939791-38-5
Molecular Formula C₂₁H₂₀F₃N₇O₃S • CH₆O₃S
Molecular Weight 665.66
Purity ≥98% by HPLC
Solubility DMSO (>20 mg/ml)
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.C1=CC=C(C=C1)S(=O)(=O)O
InChi InChI=1S/C21H20F3N7O3S.C6H6O3S/c1-31(35(2,33)34)19-12(4-3-7-25-19)10-26-18-15(21(22,23)24)11-27-20(30-18)28-14-5-6-16-13(8-14)9-17(32)29-16;7-10(8,9)6-4-2-1-3-5-6/h3-8,11H,9-10H2,1-2H3,(H,29,32)(H2,26,27,28,30);1-5H,(H,7,8,9)
InChi Key LKLWTLXTOVZFAE-UHFFFAOYSA-N
PubChem CID 16118986
Handling Protect from air and moisture
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

F-562271 is an ATP-competitive, reversible inhibitor of FAK (IC₅₀ = 1.5 nM). It displays 10-fold reduced potency for PYK2 (IC₅₀ = 14 nM) and >100-fold selectivity against other protein kinases. PF-562271 inhibits FAK phosphorylation with an EC₅₀ value of 93 ng/ml in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models.


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