BX-912

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP01898CAS No. ：702674-56-4Purity：98%

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CAS No.	702674-56-4	Cat. No.	BCP01898
Name	BX-912
Synonyms	BX912;BX 912;
SMILES
Chemical Name
Formula	C20H23BrN8O	M. Wt	471.36
Purity	98%	Storage	Store at 4-8°C
Description	BX912 prevents ChcK1, PKA, c-kit, and KDR with IC50 of 0.83, 0.11, 0.85, and 0.41 μM, resepectively. BX912 blocks PDK1/Akt signaling in tumor cells and suppresses the anchorage-dependent growth of a variety of tumor cell lines (such as PC-3 cells ) in culture or induces apoptosis. A number of cancer cell lines (such as MDA-468 breast cancer) with elevated Akt activity are >30-fold more sensitive to growth inhibition by PDK1 inhibitor BX912 in soft agar than on tissue culture plastic, consistent with the cell survival function of the PDK1/Akt signaling pathway, which is particularly important for unattached cells. BX912 potently blocks PDK1 enzyme activity in a direct kinase assay format, although BX912 fails to block preactivated AKT2 activity (IC50 > 10 μM). Therefore, BX-912 is a direct inhibitor of PDK1. BX912 is a competitive inhibitor of PDK1 activity with respect to its substrate, ATP, suggesting that BX912 binds to the ATP binding pocket of PDK1. The aminopyrimidine backbone of