1144068-46-1 Usage
Description
N-[4-[1-(1,4-Dioxaspiro[4.5]dec-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-N'-methylurea, also known as WYE-125132, is a highly potent, ATP-competitive, and specific inhibitor of the mammalian target of rapamycin (mTOR). It is a complex organic compound with a unique molecular structure that allows it to selectively bind to and inhibit the mTOR enzyme, playing a crucial role in regulating cell growth, proliferation, and survival.
Uses
Used in Pharmaceutical Industry:
N-[4-[1-(1,4-Dioxaspiro[4.5]dec-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-N'-methylurea is used as a therapeutic agent for the treatment of various diseases, including cancer, due to its ability to inhibit the mTOR pathway, which is often dysregulated in these conditions. By targeting the mTOR enzyme, WYE-125132 can help control cell growth and proliferation, leading to potential therapeutic benefits.
Used in Cancer Research:
In the field of cancer research, N-[4-[1-(1,4-Dioxaspiro[4.5]dec-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-N'-methylurea is used as a research tool to study the role of the mTOR pathway in tumor growth and progression. Its potent and specific inhibition of mTOR allows researchers to investigate the molecular mechanisms underlying cancer development and identify potential therapeutic targets.
Used in Drug Development:
N-[4-[1-(1,4-Dioxaspiro[4.5]dec-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-N'-methylurea is also used in drug development as a lead compound for the design and synthesis of new mTOR inhibitors. Its unique structure and high potency make it an attractive starting point for the development of more effective and selective mTOR inhibitors, which could have significant implications for the treatment of various diseases, including cancer.
Biological Activity
wye-125132 (wye-132) is highly potent, atp-competitive, and specific inhibitor of mtor kinase with ic50 value of 0.19±0.07nmol/l, ＞5000-fold selective versus pi3ks [1].wye-125132 (wye-132) has been reported to mtorc1-dependent phosphorylation of s6k (t389) and mtorc2-dependent phos-phorylation of akt (s473) in immune-complex assay. in addition, in insulin-like growth factor-i(igf-i)–induced rat1, the pik3ca mutant mda361, or pten-null u87mg cells, wye-125132 (wye-132) has also been revealed to dose-dependently inhibit p-s6k(t389) and p-akt(s473) with ec50 in low nanomolar range. apart from these, wye-125132 (wye-132) has shown a potent anti-proliferative agent against mda361, pc3mm2, u87mg, a549, and hct116 cell lines. moreover, wye-125132 (wye-132) has noted a stronger inhibition of protein synthesis and cell size in mda361 and hek293 cell lines [1].
references
[1] yu k1, shi c, toral-barza l, lucas j, shor b, kim je, zhang wg, mahoney r, gaydos c, tardio l, kim sk, conant r, curran k, kaplan j, verheijen j, ayral-kaloustian s, mansour ts, abraham rt, zask a, gibbons jj. beyond rapalog therapy: preclinical pharmacology and antitumor activity of wye-125132, an atp-competitive and specific inhibitor of mtorc1 and mtorc2. cancer res. 2010 jan 15;70(2):621-31. doi: 10.1158/0008-5472.can-09-2340. epub 2010 jan 12.
Check Digit Verification of cas no
The CAS Registry Mumber 1144068-46-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,4,4,0,6 and 8 respectively; the second part has 2 digits, 4 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1144068-46:
(9*1)+(8*1)+(7*4)+(6*4)+(5*0)+(4*6)+(3*8)+(2*4)+(1*6)=131
131 % 10 = 1
So 1144068-46-1 is a valid CAS Registry Number.
1144068-46-1Relevant articles and documents
Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituent
Curran, Kevin J.,Verheijen, Jeroen C.,Kaplan, Joshua,Richard, David J.,Toral-Barza, Lourdes,Hollander, Irwin,Lucas, Judy,Ayral-Kaloustian, Semiramis,Yu, Ker,Zask, Arie
scheme or table, p. 1440 - 1444 (2010/07/06)
A series of pyrazolopyrimidine mammalian Target Of Rapamycin (mTOR) inhibitors with various substituents at the 1-position have been prepared, resulting in compounds with excellent potency, selectivity and microsomal stability. Combination of a 1-cyclohexyl ketal group with a 2,6-ethylene bridged morpholine in the 4-position and a ureidophenyl group in the 6-positon resulted in compound 8a, that selectively suppressed key mTOR biomarkers in vivo for at least 8 h following iv administration and showed excellent oral activity in a xenograft tumor model.
