PD 166285An inhibitor of RTK, c-Src, FGFR1, Wee 1, and PDGFRβ

PD 166285 (CAS 212391-63-4)

PD 166285 | CAS 212391-63-4 is rated 5.0 out of 5 by 1.
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Synonym: Heparin-Cantithrombin II
Application: An inhibitor of RTK, c-Src, FGFR1, Wee 1, and PDGFRβ
CAS Number: 212391-63-4
Purity: ≥98%
Molecular Weight: 585.35
Molecular Formula: C26H27Cl2N5O22HCl
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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PD 166285 is a potent inhibitor of the tyrosine kinases c-Src, Flg (fibroblast growth factor receptor 1, FGFR1), and PDGFRβ (platelet-derived growth factor receptor β) (IC50 values are 8.4, 39.3 and 98.3 nM respectively). PD 166285 also inhibits the checkpoint kinases Wee1 and MYT1 (Myt1), abolishes Cdc2 phosphorylation in numerous tumor cell lines, and abrogates the G2 checkpoint. PD 166285 is an RTK inhibitor with broad-spectrum properties and displays anti-angiogenic activity and anti-tumor efficacy when used with PDT (photodynamic therapy). PD 166285 is an inhibitor of EGFR.


References

Star, W., et al.: Cancer Res., 46, 2532 (1986), Sawutz, D., et al.: Biochem. Pharm., 51, 1631 (1996), Voest, E., et al.: Anti-Cancer Drugs, 7, 723 (1996), Connolly, C., et al.: Bioorg. Med. Chem. Lett., 7(18), 2415 (1997), Hamby, J., et al.: J. Med. Chem., 40, 2296 (1997)

Physical State :
Solid
Solubility :
Soluble in water, methanol, and DMSO (100 mM).
Storage :
Store at 4° C
Melting Point :
236-241° C
Refractive Index :
n20D ~1.64 (Predicted)
IC50 :
c-Src: IC50 = 8.4 nM; Wee 1: IC50 = 24 nM; Flg: IC50 = 39.3 nM; MYT1: IC50 = 72 nM; EGFR: IC50 = 87.5 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
9916391
MDL Number :
MFCD18086890
SMILES :
CCN(CC)CCOC1=CC=C(C=C1)NC2=NC=C3C=C(C(=O)N(C3=N2)C)C4=C(C=CC=C4Cl)Cl.Cl.Cl

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Certificate of Analysis

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PD 166285  Product Citations

See how others have used PD 166285. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 24229357  Rohe, A. et al. 2014. Assay Drug Dev Technol. 12: 136-44.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Leijen Leijen, S. et al. (PubMed 20406171) reported that abrogation of the G2 checkpoint by inhibition of Wee-1 kinase by PD 166285 results in sensitization of p53-deficient tumor cells to DNA-damaging agents. -SCBT Publication Review
Date published: 2015-04-11
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