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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Purity: ≥98%
PF-573228 (PF573228) is a selective and ATP-competitive FAK (focal adhesion kinase) inhibitor with potential antitumor activity. It inhibits FAK with an IC50 of 4 nM in a cell-free assay, and is ~50- to 250-fold more selective for FAK over other kinases including Pyk2, CDK1/7 and GSK-3β. PF-573228 shows high in vivo antitumor efficacy in PC3M-luc-C6 xenograft models. FAK is a non-receptor protein-tyrosine kinase that regulates integrin and growth factor signaling pathways involved in cell migration, proliferation, and survival. FAK is over expressed in many cancers, including breast and prostate cancer.
ln Vitro |
PF-573228 suppresses the purified recombinant catalytic portion of FAK with an IC50 of 4 nM [1]. PF-573228 suppresses FAK phosphorylation on Tyr397 at an IC50 of 30-100 nM[1]. PF-573228 significantly lowers FAK Tyr397 phosphorylation [1]. PF-573228 decreases chemotaxis and chemotactic migration while also reducing focal adhesion turnover [1].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Slack-Davis JK, et al. Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52
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Molecular Formula |
C22H20F3N5O3S
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Molecular Weight |
491.49
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CAS # |
869288-64-2
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Related CAS # |
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SMILES |
S(C([H])([H])[H])(C1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])N([H])C1C(C(F)(F)F)=C([H])N=C(N=1)N([H])C1C([H])=C([H])C2=C(C=1[H])C([H])([H])C([H])([H])C(N2[H])=O)(=O)=O
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Chemical Name |
3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone
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Synonyms |
PF573,228; PF 573,228; PF-573,228; PF573228; PF 573228; PF-573228;
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.09 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% propylene glycol:30 mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0346 mL | 10.1731 mL | 20.3463 mL | |
5 mM | 0.4069 mL | 2.0346 mL | 4.0693 mL | |
10 mM | 0.2035 mL | 1.0173 mL | 2.0346 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.