Biological Activity
Potent and selective breast tumor kinase (Brk) inhibitor (IC50 = 30 nM). Exhibits >650-fold selectively for Brk over Aurora B kinase and Lck. Downregulates SNAIL protein, restores E-cadherin expression and suppresses migration in breast cancer cells. Also active in vivo and orally bioavailable.
Technical Data
| M. Wt | 483.93 |
| Formula | C23H22FN7O2.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| InChI Key | GWHGHKMCIUENCZ-UHFFFAOYSA-N |
| Smiles | Cl.FC1=C(NC2=NC(=CN3C(=CN=C23)C2=CNN=C2)C2CC2)C=CC(=C1)C(=O)N1CCOCC1 |
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 | 48.39 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 483.93. 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 | 2.07 mL | 10.33 mL | 20.66 mL |
| 5 mM | 0.41 mL | 2.07 mL | 4.13 mL |
| 10 mM | 0.21 mL | 1.03 mL | 2.07 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.41 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Zeng et al (2011) Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors. Bioorg.Med.Chem.Lett 21 5870 PMID: 21855335
Ito et al (2016) PTK6 inhibition suppresses metastases of triple-negative breast cancer via SNAIL-dependent E-cadherin regulation. Cancer Res. 76 4406 PMID: 27302163
Keywords: P21d hydrochloride, supplier, Potent, selective, breast, tumor, kinase, Brk, PTK6, inhibitors, inhibits, orally, bioavailable, Src, Kinases, Tocris Bioscience
