PD 180970

Cat. No. 4965

PD 180970 C21H15Cl2FN4O [287204-45-9]

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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).

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Corbin et al (2004) Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970. Blood 104 3754. PMID: 15304388.

La Rosée et al (2002) Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571). Cancer Res. 62 7149. PMID: 12499247.

Dorsey et al (2000) The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210bcr-abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Cancer Res. 60 3127. PMID: 10866298.

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Keywords: PD 180970, supplier, PD180970, Pfizer, Bcr-Abl, tyrosine, kinase, inhibitors, inhibits, c-Src, KIT, Tocris Bioscience, Abl Kinase Inhibitor products

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