PP121 has been shown to be an inhibitor of tyrosine and phosphoinositide kinases. PP121 inhibits c-Abl (IC50 of 18 nM), PI 3-kinase (IC50 of < 0.06 μM), PDGFR (IC50 of 2 nM), Hck (IC50 of 8 nM), FRAP (IC50 of 10 nM), Flk-1 (IC50 of 12 nM), SRC (IC50 of 14 nM), and DNA-PK (IC50 of < 0.06 μM). PP121 does not affect other serine-threonine protein kinases. PP-121 potently inhibits the proliferation of a subset of tumor cell lines by direct inhibition of PI 3-kinase and FRAP.
Soluble in DMSO (64 mg/mL at 25° C), water (<1 mg/mL at 25° C), and ethanol (2 mg/mL at 25° C).
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