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| 25mg |
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Purity: ≥98%
PF-00562271 besylate (also called PF562271 or PF-562271 Besylate), the benzenesulfonate salt form of PF-00562271, is an ATP-competitive and orally bioavailable inhibitor of FAK (focal adhesion kinase) and Pyk2 catalytic activity with potential antitumor activity. It inhibits FAK and Pyk2 with IC50s of 1.5 and 14 nmol/L, respectively. It demonstrates high in vivo antitumor efficacy against multiple human xenograft models.
| ln Vitro |
In recombinant enzyme tests, PF-562271 (VS-6062) besylate is a 30- to 120-nM (15.2 to 60.1 ng/mL) inhibitor of cdk2/E, cdk5/p35, cdk1/B, and cdk3/E[1]. PF-562,271 inhibits the formation of new blood vessels in response to bFGF in chicken chorioallantoic membrane assays[2]. It has been shown that PF-562,271 treatment or siRNA-mediated knockdown of FAK strengthens cell-cell adhesions[3].
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| ln Vivo |
In tumor-bearing mice, PF-562,271 (33 mg/kg, po) reduces FAK phosphorylation in tumors in a way that is dependent on both dose and time. PF-562,271's total blood concentration is inhibited by FAK phosphorylation, resulting in an estimated EC50 of 93 ng/mL. On day three, treated tumors treated with PF-562,271 (25 mg/kg, po) exhibit a 2-fold increase in apoptosis in comparison to control tumors treated with vehicle[1]. Dasatinib and PF-562,271 (33 mg/kg, po) significantly restrict the ability of tumor cells to migrate within the mice. E-cadherin dynamics are changed in vivo when PF-562,271 therapy inhibits FAK kinase activity[3].
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| Additional Infomation |
FAK Inhibitor PF-00562271 is an orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities. FAK inhibitor PF-00562271 inhibits the tyrosine kinase FAK, and to a lesser extent, proline-rich tyrosine kinase (PYK2), which may inhibit tumor cell migration, proliferation, and survival. As FAK is a signal transducer for integrins, inhibition of FAK by this agent may prevent integrin-mediated activation of several downstream signals including ERK, JNK/MAPK and PI3K/Akt. FAK and PYK2, upregulated in many tumor cell types, are involved in tumor cell invasion, migration and proliferation.
See also: PF-562271 (annotation moved to). |
| Molecular Formula |
C21H20F3N7O3S.C6H6O3S
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|---|---|
| Molecular Weight |
665.66
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| Exact Mass |
665.133
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| CAS # |
939791-38-5
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| Related CAS # |
PF-562271;717907-75-0
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| PubChem CID |
16118986
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
6.515
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
45
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| Complexity |
1040
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LKLWTLXTOVZFAE-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
N-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide benzenesulfonate
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| Synonyms |
PF-562271; PF-562271 Besylate; PF562271; PF-00562271; PF00562271; PF 00562271; PF562271 PhSO3H; PF562271 benzesulfonate salt; PF-271; PF271; PF271
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: ≥ 1.67 mg/mL (2.51 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 16.7 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. Solubility in Formulation 2: ≥ 1.67 mg/mL (2.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 16.7 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. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (2.51 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: 4% DMSO+30% PEG 300+ddH2O:3 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5023 mL | 7.5113 mL | 15.0227 mL | |
| 5 mM | 0.3005 mL | 1.5023 mL | 3.0045 mL | |
| 10 mM | 0.1502 mL | 0.7511 mL | 1.5023 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.
Efficacy of PF-562,271 in PC3M-luc-C6 subcutaneuous local implant xenograft model: PF-562,271 was administered at 25 mg/kg P.O. BID 5x/wk for two weeks.Cancer Biol Ther.2010Jul 1;10(1):38-43. |
(A) Bioluminescent image time course of an intracardiac inoculated vehicle control mouse. Vehicle was administered P.O. BID 5x/wk for three weeks. (B) Bioluminescent image time course of an intracardiac inoculated treated with PF-562,271. PF-562,271 was administered at 25 mg/kg P.O. BID 5x/wk for three weeks. Cancer Biol Ther. 2010 Jul 1; 10(1): 38–43. |
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