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[CAS NO. 939791-38-5] PF-562271 besylate
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-10458 |
| Brand: | MCE |
| CAS: | 939791-38-5 |
Overview
| MDL | MFCD14105612 |
|---|---|
| Molecular Weight | 665.66 |
| Molecular Formula | C27H26F3N7O6S2 |
| SMILES | CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O.O=S(C5=CC=CC=C5)(O)=O |
12 Publications Citing Use of MCE
- [1]Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
- [2]Clin Cancer Res. 2019 Jul 15;25(14):4552-4566.
- [3]Cancer Res. 2013 May 1;73(9):2873-83.
- [4]Cell Death Dis. 2022 Sep 10;13(9):783.
- [5]Cell Discov. 2022 Sep 6;8(1):84.
- [6]Int J Cancer. 2015 Oct 1;137(7):1549-59.
- [7]Sci Rep. 2018 May 8;8(1):7228.
- [8]Life Sci. 2021 Jan 25;119112.
- [9]J Nat Med. 2020 Sep;74(4):732-740.
- [10]Research Square Preprint. 2021 Dec.
- [11]Practical Oncology Journal. 2015, 29(5): 444-449.
- [12]Harvard Medical School LINCS LIBRARY
Summary
IC50 & Target
IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3) [1]
In Vitro
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 in recombinant enzyme assays [1] . PF-562,271 blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays [2] . Treatment of cells with PF-562,271 or knock-down of FAK by siRNA is observed to increase cell-cell adhesion strength [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC 50 of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3 [1] . PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 21.4 mg/mL ( 32.15 mM ; Need ultrasonic and warming)
H 2 O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [1] Roberts WG, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res, 2008, 68(6), 1935-1944.
- [2] Lim ST, et al. FERM control of FAK function: implications for cancer therapy. Cell Cycle, 2008, 7(15), 2306-2314.
- [3] Canel M, et al. Quantitative in vivo imaging of the effects of inhibiting integrin signaling via Src and FAK on cancer cell movement: effects on E-cadherin dynamics. Cancer Res, 2010, 70(22), 9413-9422.
Synonyms
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