Biological Activity
Potent inhibitor of the tyrosine kinases c-Src, fibroblast growth factor receptor 1 (FGFR1), and platelet-derived growth factor receptor β (PDGFRβ) (IC50 values are 8.4, 39.3 and 98.3 nM respectively). Also inhibits the checkpoint kinases Wee1 and Myt1; abolishes Cdc2 phosphorylation in numerous tumor cell lines and abrogates the G2 checkpoint.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries
PD 166285 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 585.35 |
| Formula | C26H27Cl2N5O2.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 212391-63-4 |
| PubChem ID | 9916391 |
| InChI Key | NADLBPWBFGTESN-UHFFFAOYSA-N |
| Smiles | CN(C1=NC(NC4=CC=C(OCCN(CC)CC)C=C4)=NC=C1C=C2C3=C(Cl)C=CC=C3Cl)C2=O.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 58.53 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 585.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.71 mL | 8.54 mL | 17.08 mL |
| 5 mM | 0.34 mL | 1.71 mL | 3.42 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.71 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Panek et al (1997) In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor. J.Pharmacol.Exp.Ther. 283 1433 PMID: 9400019
Wang et al (2001) Radiosensitization of p53 mutant cells by PD0166285, a novel G2 checkpoint abrogator. Cancer Res. 61 8211 PMID: 11719452
Hashimoto et al (2006) Cell cycle regulation by the Wee1 inhibitor PD0166285, Pyrido [2,3-d] pyimidine, in the B16 mouse melanoma cell line. BMC Cancer 6 292 PMID: 17177986
Keywords: PD 166285 dihydrochloride, supplier, Src, FGFR, PDGFRbeta, PDGFRb, PDGFRβ, PDGFR, Wee1, inhibitors, inhibits, Pfizer, RTKs, receptor, tyrosine, kinases, fibroblast, platelet, growth, factors, PD166285, Src, Kinases, FGFR, PDGFR, Checkpoint, Control, Kinases, Src, Kinases, Tocris Bioscience
