PD 166285 dihydrochloride

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Cat.No. 3785 - PD 166285 dihydrochloride | C26H27Cl2N5O2.2HCl | CAS No. 212391-63-4
Description: Potent Src inhibitor; also inhibits FGFR1, PDGFRβ and Wee1
Chemical Name: 6-(2,6-Dichlorophenyl)-2-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 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

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References

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


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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

1 Citation for PD 166285 dihydrochloride

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


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