PD 166285 dihydrochloride

Catalog # Availability Size / Price Qty
3785/1
3785/10
PD 166285 dihydrochloride | CAS No. 212391-63-4 | Src Family Kinase Inhibitors
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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%

Product Details
Citations (2)
Supplemental Products
Reviews

Biological Activity

PD 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.

Technical Data

M.Wt:
585.35
Formula:
C26H27Cl2N5O2.2HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Desiccate at RT
CAS No:
212391-63-4

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.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.

Background References

  1. Loss-of-function mutations in ATP6AP1 and ATP6AP2 in granular cell tumors
    F Pareja, AH Brandes, T Basili, P Selenica, FC Geyer, D Fan, A Da Cruz Pa, R Kumar, DN Brown, R Gularte-Mé, B Alemar, R Bi, RS Lim, I de Bruijn, S Fujisawa, R Gardner, E Feng, A Li, EM da Silva, JR Lozada, P Blecua, L Cohen-Goul, AA Jungbluth, EA Rakha, IO Ellis, MIA Edelweiss, J Palazzo, L Norton, T Hollmann, M Edelweiss, BP Rubin, B Weigelt, JS Reis-Filho
    Nat Commun, 2018;9(1):3533.
  2. In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor.
    Panek et al.
    J.Pharmacol.Exp.Ther., 1997;283:1433
  3. Radiosensitization of p53 mutant cells by PD0166285, a novel G2 checkpoint abrogator.
    Wang et al.
    Cancer Res., 2001;61:8211
  4. Cell cycle regulation by the Wee1 inhibitor PD0166285, Pyrido [2,3-d] pyimidine, in the B16 mouse melanoma cell line.
    Hashimoto et al.
    BMC Cancer, 2006;6:292

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Citations for PD 166285 dihydrochloride

The citations listed below are publications that use Tocris products. Selected citations for PD 166285 dihydrochloride include:

2 Citations: Showing 1 - 2

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