Catalog Number: 4965
Chemical Name: 6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
Biological Activity
ATP-competitive inhibitor of p210bcr/abl tyrosine kinase; selectively induces apoptosis in chronic myeloid leukemia (CML) K562 cells. Inhibits in vivo tyrosine phosphorylation of Gab2, CrkL and p210bcr/abl (IC50 values are 80, 80 and 170 nM respectively). Potently inhibits p210bcr/abl autophosphorylation in vitro (IC50 = 5 nM). Also potently inhibits c-Src and KIT (IC50 values are 0.8 and 50 nM, respectively).
Technical Data
  • M.Wt:
    429.27
  • Formula:
    C21H15Cl2FN4O
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    287204-45-9
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210bcr-abl tyrosine kinase and induces apoptosis of K562 leukemic cells.
    Dorsey et al.
    Cancer Res., 2000;60:3127
  2. Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970.
    Corbin et al.
    Blood, 2004;104:3754
  3. Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571).
    La Rosée et al.
    Cancer Res., 2002;62:7149

Have you used PD 180970?

Submit a review and receive a $25US/€18/£15/$25CAN amazon gift card if you include an image - $10US/€7/£6/$10CAN Amazon card for reviews without an image. Limited to verified customers in USA, Canada and Europe.

Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details

Note:

Contact Information

Calculators

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

R&D Systems Guarantee

Feedback

Customer Information