[CAS NO. 939791-41-0] PF-562271 HCl
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PRODUCTS SPECIFICATIONS [939791-41-0]
Store
Catalog
SLK-S7357
Brand
Selleck
CAS
939791-41-0
DESCRIPTION [939791-41-0]
Overview
| MDL | MFCD17170115 |
|---|---|
| Molecular Weight | 543.95 |
| Molecular Formula | C21H21ClF3N7O3S |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8384 mL | 9.1920 mL | 18.3840 mL |
| 5 mM | 0.3677 mL | 1.8384 mL | 3.6768 mL |
| 10 mM | 0.1838 mL | 0.9192 mL | 1.8384 mL |
| 50 mM | 0.0368 mL | 0.1838 mL | 0.3677 mL |
Description
PF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of with 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.
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
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
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