DESCRIPTION
The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin) and regulate different pathways. PP242 is an inhibitor of the active site of mTOR kinase in both mTORC1 and mTORC2 (IC50 = 8 nM).1,2 It less effectively inhibits PKCñ, PI3-kinase subunit p110ó, JAK2, PKCòI, and PKCòII (IC50 = 49, 102, 110, 198, and 185, respectively).2,3 PP242 has been shown to cause the death of certain human and murine leukemia cells more potently than rapamycin and, in vivo, delays leukemia onset and augments the effects of tyrosine kinase inhibitors in suppressing leukemic expansion and extending survival.4
TECHNICAL INFORMATION
Formal Name
2-[4-amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
CAS Number
1092351-67-1
Molecular Formula
C16H16N6O
Formula Weight
308.3
Purity
âÂÂ¥95%
Formulation
A crystalline solid
SHIPPING & STORAGE
Storage
-20ðC
Shipping
Room temperature in continental US; may vary elsewhere
Stability
âÂÂ¥ 2 years