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Submit ReviewPD 166285 dihydrochloride is a 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.
Sold for research purposes under agreement from Pfizer Inc.
PD 166285 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 58.53 | 100 |
The following data is based on the product molecular weight 585.35. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for PD 166285 dihydrochloride, please let us know.
Keywords: PD 166285 dihydrochloride, PD 166285 dihydrochloride supplier, Src, FGFR, PDGFRbeta, PDGFRb, PDGFRβ, PDGFR, Wee1, inhibitors, inhibits, Pfizer, RTKs, receptor, tyrosine, kinases, fibroblast, platelet, growth, factors, PD166285, Kinases, Checkpoint, Control, 3785, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for PD 166285 dihydrochloride include:
Gaffré et al (2011) A critical balance between Cyclin B synthesis and Myt1 activity controls meiosis entry in Xenopus oocytes. Toxicol Lett 138 3735 PMID: 21795279
Hui et al (2021) Echinoderm Microtubule Associated Protein Like 1 Is Indispensable for Oocyte Spindle Assembly and Meiotic Progression in Mice. Front Cell Dev Biol 9 687522 PMID: 34124073
Do you know of a great paper that uses PD 166285 dihydrochloride from Tocris? Please let us know.
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