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[CAS NO. 717907-75-0] PF-562271
| 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-10459 |
| Brand: | MCE |
| CAS: | 717907-75-0 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 507.49 |
| Molecular Formula | C21H20F3N7O3S |
| SMILES | CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(C=C3)NC(C4)=O)=NC=C2C(F)(F)F)=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) is shown to be a 30- to 120-nM inhibitor of CDK2/E, CDK5/p35, CDK1/B, and CDK3/E in recombinant enzyme assays, in cell-based assays evaluating the role of CDKs, a 48-hour exposure of 3.3 μM PF-562271 is required to alter cell cycle progression. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with a IC
50
of 5 nM
[1]
.
PF-562271, a selective inhibitor of both FAK and proline-rich tyrosine kinase 2 (PYK2), a FAK-related family member, on cell growth and colony formation in Ewing sarcoma cell lines. Seven cell lines are treated for 5 days with PF-562271 across a range of concentrations using 2-fold serial dilutions. Treatment with PF-562271 impaires cell viability in all cell lines, with an average IC
50
of 2.4 μM after 3 days of treatment. TC32 and A673 are the 2 most sensitive cell lines, with IC
50
concentrations of 2.1 and 1.7 μM, respectively
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PF-562271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC 50 of 93 ng/mL, total) after p.o. administration to tumor-bearing mice [1] . Rats that receive PF-562271 demonstrate a decrease in tumor growth after 2 weeks of treatment with signs of bone healing as evidenced by the deposition of new bone (cortical and cancellous) at sites previously damaged by the tumor [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
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 246.31 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9705 mL | 9.8524 mL | 19.7048 mL |
| 5 mM | 0.3941 mL | 1.9705 mL | 3.9410 mL |
| 10 mM | 0.1970 mL | 0.9852 mL | 1.9705 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1.67 mg/mL (3.29 mM); Clear solution
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] Crompton BD, et al. High-throughput tyrosine kinase activity profiling identifies FAK as a candidate therapeutic target in Ewing sarcoma. Cancer Res. 2013 May 1;73(9):2873-83.
- [3] Bagi CM, et al. Dual focal adhesion kinase/Pyk2 inhibitor has positive effects on bone tumors: implications for bone metastases. Cancer. 2008 May 15;112(10):2313-21.
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