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
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 Basic information
- Product Name:
- 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
- Synonyms:
-
- 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
- WYE 125132
- WYE 125132(WYE-132)
- 1-(4-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-1-(1,4-dioxaspiro[4.5]decan-8-yl)-1H-pyrazolo[3,4-d]pyriMidin-6-yl)phenyl)-3-Methylurea
- WYE125132/WYE-125132/WYE-132
- Urea, 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'-methyl-
- 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 WYE125132(WYE-132)
- WYE 125132 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
- CAS:
- 1144068-46-1
- MF:
- C27H33N7O4
- MW:
- 519.6
- Product Categories:
-
- mTOR
- PI3K
- PI3K/Akt/mTOR
- Inhibitors
- Akt
- Mol File:
- 1144068-46-1.mol
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 Chemical Properties
- Melting point:
- 162-184°C (dec.)
- Density
- 1.55
- storage temp.
- -20°C Freezer
- solubility
- DMSO (Slightly)
- form
- White powder solid.
- pka
- 13.82±0.46(Predicted)
- color
- Off-White to Pale Beige
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 Usage And Synthesis
Uses
WYE-125132 is a highly potent, ATP-competitive and specific mammalian target of rapamycin (mTOR) inhibitor.
Definition
ChEBI: 1-[4-[1-(1,4-dioxaspiro[4.5]decan-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-6-pyrazolo[3,4-d]pyrimidinyl]phenyl]-3-methylurea is a member of ureas.
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].
target
mTOR
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.
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'-methylureaSupplier
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