1092351-67-1 Usage
Description
PP242 is a potent inhibitor of the mammalian target of rapamycin (mTOR), a serine-threonine kinase that plays a central role in two protein complexes, mTORC1 and mTORC2. It is a member of the class of pyrazolopyrimidines and exhibits anti-cancer properties by inhibiting the active site of mTOR kinase in both mTORC1 and mTORC2.
Uses
Used in Leukemia Therapy:
PP242 is used as a dual mTORC1/C2 inhibitor for leukemia therapy, suppressing mTOR signaling. It has been shown to cause the death of certain human and murine leukemia cells more potently than rapamycin. In vivo, PP242 delays leukemia onset and augments the effects of tyrosine kinase inhibitors in suppressing leukemic expansion and extending survival.
Enzyme inhibitor
This ATP-competitive mTORC1/mTORC2 inhibitor (FW = 308.34 g/mol; CAS 1092351-67-1; Solubility: 25 mM in DMSO), also named 2-[4-amino- 1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol, has a IC50 = 8 nM for both isoforms of mammalian target of rapamycin (mTOR), also known as FK506-binding protein 12-rapamycin-associated protein 1, or FRAP1, a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, autophagy, and transcription. PP-242 shows considerable selectivity for mTOR versus PI3K family kinases. In models of acute leukemia harboring the Philadelphia chromosome (Ph) translocation, PP242, but not rapamycin, causes death of mouse and human leukemia cells. Indeed, PP242 completely inhibits TORC1 and TORC2 signaling in BCR-ABL+ cells, whereas rapamycin partially suppresses TORC1 and drives a PI3K/AKT surge. Moreover, PP242 augments TNF-related apoptosis-inducing ligand- (TRAIL-) induced apoptosis in NSCLC cells, indicating that mTORC2 regulates Cbl-dependent FLIPS degradation and TRAIL-induced apoptosis Other Targets: p110γ (IC50 = 0.102 μM); DNA-PK ((IC50 = 0.408 μM); p110δ ((IC50 = 1.27 μM); p110α ((IC50 = 1.96 μM), and p110β ((IC50 = 2.2 μM), with much weaker inhibition of 215 other kinases.
Check Digit Verification of cas no
The CAS Registry Mumber 1092351-67-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,9,2,3,5 and 1 respectively; the second part has 2 digits, 6 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1092351-67:
(9*1)+(8*0)+(7*9)+(6*2)+(5*3)+(4*5)+(3*1)+(2*6)+(1*7)=141
141 % 10 = 1
So 1092351-67-1 is a valid CAS Registry Number.