PF-562271 717907-75-0
Product Description
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Molecular Weight:
507.49 PF-562271 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.
Biological Activity
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.
PF-562271 ( 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.
Protocol(Only for Reference)
Kinase Assay: [1]
Animal Study: [1]
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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
Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on 717907-75-0. We are ready to answer your questions on packaging, logistics, certification or any Other aspects about PF-562271 717907-75-0、717907-75-0 PF-562271. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight:
507.49 PF-562271 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.
Biological Activity
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.
PF-562271 ( 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.
Protocol(Only for Reference)
Kinase Assay: [1]
Recombinant kinase assay | Purified-activated FAK kinase domain (410–689 aa) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl2 for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2 mol/L H2SO4). IC50 values are determined using the Hill-Slope Model. |
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Animal Study: [1]
Animal Models | Athymic female mice bearing BxPc3 or PC3-M xenografts. | ||
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Formulation | 5% Gelucire | ||
Dosages | 50 mg/kg | ||
Administration | Oral gavage | ||
Solubility | 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL | ||
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species | Baboon | Dog | Monkey | Rabbit | Guinea pig | Rat | Hamster | Mouse |
Weight (kg) | 12 | 10 | 3 | 1.8 | 0.4 | 0.15 | 0.08 | 0.02 |
Body Surface Area (m2) | 0.6 | 0.5 | 0.24 | 0.15 | 0.05 | 0.025 | 0.02 | 0.007 |
Km factor | 20 | 20 | 12 | 12 | 8 | 6 | 5 | 3 |
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.
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × | mouse Km(3) | = 11.2 mg/kg |
rat Km(6) |
Chemical Information
Molecular Weight (MW) | 507.49 |
---|---|
Formula | C21H20F3N7O3S |
CAS No. | 717907-75-0 |
Storage | 3 years -20℃Powder |
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6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | |
Solubility (25°C) * | In vitro | DMSO | 101 mg/mL (199.01 mM) |
---|---|---|---|
Water | <1 mg/mL ( | ||
Ethanol | <1 mg/mL ( | ||
In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol | 30 mg/mL | |
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Chemical Name | Methanesulfonamide, N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl- |
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Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on 717907-75-0. We are ready to answer your questions on packaging, logistics, certification or any Other aspects about PF-562271 717907-75-0、717907-75-0 PF-562271. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Angiogenesis > FAK Inhibitor
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