PD 180970

Pricing Availability   Qty
Cat.No. 4965 - PD 180970 | C21H15Cl2FN4O | CAS No. 287204-45-9
Description: p210Bcr/Abl kinase inhibitor; also inhibits c-Src and KIT
Chemical Name: 6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
Purity: ≥98% (HPLC)

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
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 287204-45-9
PubChem ID 5311104
Smiles CN(C(C(C4=C(Cl)C=CC=C4Cl)=C3)=O)C1=C3C=NC(NC2=CC(C)=C(F)C=C2)=N1

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
DMSO 21.46 50

Preparing Stock Solutions

The following data is based on the product molecular weight 429.27. 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
0.5 mM 4.66 mL 23.3 mL 46.59 mL
2.5 mM 0.93 mL 4.66 mL 9.32 mL
5 mM 0.47 mL 2.33 mL 4.66 mL
25 mM 0.09 mL 0.47 mL 0.93 mL

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References are publications that support the biological activity of the product.

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

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

If you know of a relevant reference for PD 180970, please let us know.

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