|
| | 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 | | EINECS: | | | 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 Structure](CAS2/GIF/1144068-46-1.gif) |
| | 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'-methylurea Preparation Products And Raw materials |
|
