BX-912 is an aminopyrimidine-based, ATP-competitive inhibitor of PDK1 at an IC50 of 12 nM. In a panel of relevant serine-threonine and receptor-tyrosine kinases, BX-912 showed at least 20-fold selectivity with the exception of 9-fold selectivity (110 nM) for PKA. In a panel of cell lines, BX-912 potently inhibits growth of PC-3 cells in soft agar at an IC50 of 320 nM. (1)
Technical information:
| Chemical Formula: | C20H23BrN8O | |
| CAS #: | 702674-56-4 | |
| Molecular Weight: | 471.35 | |
| Purity: | > 98% | |
| Appearance: | white | |
| Chemical Name: | N-(3-(4-(2-(1H-imidazol-5-yl)ethylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | BX-912, BX 912, BX912 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Feldman et al., Novel Small Molecule Inhibitors of 3-Phosphoinositide-dependent Kinase-1, J. Biol. Chem. 2005, 280, 19867-19874. Pubmed ID: 15772071 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
