PF-573228 869288-64-2
Product Description
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Molecular Weight:
491.49 PF-573228 is an ATP-Competitive Inhibitor of FAK with IC50 of 4 nM, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β.
Biological Activity
PF 573228 blocks the phosphorylation of FAK Tyr397 in REF52
cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of
30-500 nM. However, PF 573228 (1 μM) with 80% inhibition of FAK
phosphorylation fails to inhibit cell growth or Apoptosis. Similar
treatment of cells with PF-228 resulted in inhibition of serum or
FN-directed migration and decreased focal adhesion turnover.
Protocol(Only for Reference)
Kinase Assay: [1]
Cell Assay: [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
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Contact us if you need more details on 869288-64-2. We are ready to answer your questions on packaging, logistics, certification or any other aspects about PF-573228 869288-64-2、869288-64-2 PF-573228. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight:
491.49 PF-573228 is an ATP-Competitive Inhibitor of FAK with IC50 of 4 nM, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β.
Biological Activity
PF 573228 blocks the phosphorylation of FAK Tyr397 in REF52
cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of
30-500 nM. However, PF 573228 (1 μM) with 80% inhibition of FAK
phosphorylation fails to inhibit cell growth or Apoptosis. Similar
treatment of cells with PF-228 resulted in inhibition of serum or
FN-directed migration and decreased focal adhesion turnover.
Protocol(Only for Reference)
Kinase Assay: [1]
Affinity determination | Purified activated FAK kinase domain (Amino Acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3', 5, 5'-tetramethylbenzidine is added, and Optical Density readings at 450 nm are obtained following the addition of stop solution (2 M H2SO4). The IC50 values are determined using the Hill slope model. |
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Cell Assay: [1]
Cell lines | REF52 or PC3 cells |
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Concentrations | ~10 μM |
Incubation Time | 3 days |
Method | Growth assays are performed by seeding 1 × 104 REF52 or PC3 cells/well of a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor for 3 days. Subsequently, the cells are harvested and counted. |
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) | 491.49 |
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Formula | C22H20F3N5O3S |
CAS No. | 869288-64-2 |
Storage | 3 years -20℃Powder |
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6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | |
Solubility (25°C) * | In vitro | DMSO | 26 mg/mL (52.9 mM) |
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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 | 2(1H)-Quinolinone, 3,4-dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]- |
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Molarity Calculator
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Contact us if you need more details on 869288-64-2. We are ready to answer your questions on packaging, logistics, certification or any other aspects about PF-573228 869288-64-2、869288-64-2 PF-573228. 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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