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 |
| InChI Key | SLCFEJAMCRLYRG-UHFFFAOYSA-N |
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.33 mL | 11.65 mL | 23.3 mL |
| 5 mM | 0.47 mL | 2.33 mL | 4.66 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.33 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
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References
References are publications that support the products' biological activity.
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
Keywords: PD 180970, supplier, PD180970, Pfizer, Bcr-Abl, tyrosine, kinase, inhibitors, inhibits, c-Src, KIT, Abl, Kinase, Src, Kinases, Other, RTKs, Abl, Kinase, Tocris Bioscience
