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)

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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

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Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution at -20^oC.

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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

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Other Information:

Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.

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