1144068-46-1
WYE-125132 (WYE-132)
CAS: 1144068-46-1
Molecular Formula: C27H33N7O4
1144068-46-1 - Names and Identifiers
| Name | WYE-125132 (WYE-132) |
| Synonyms | WYE 125132 WYE 125132(WYE-132) WYE-125132 (WYE-132) 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 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- 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 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 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) |
| CAS | 1144068-46-1 |
1144068-46-1 - Physico-chemical Properties
| Molecular Formula | C27H33N7O4 |
| Molar Mass | 519.6 |
| Density | 1.55 |
| Melting Point | 162-184°C (dec.) |
| Solubility | DMSO (Slightly) |
| Appearance | White powder solid. |
| Color | Off-White to Pale Beige |
| pKa | 13.82±0.46(Predicted) |
| Storage Condition | -20°C Freezer |
| In vitro study | WYE-125132 potently and ATP-competitively inhibits recombinant mTOR kinase with IC50 of 0.19 nM and also shows the high selectivity over various PI3Ks and a panel of 230 protein kinases. In vitro, WYE-125132 exhibits a significant anti-proliferative activity against a panel of tumor cell lines with IC50 ranging from 2 nM (LNCap) to 380 nM (HTC116). Besides, WYE-125132 also causes cell cycle progression, induction of apoptosis, and inhibition of protein synthesis and cell size. WYE-125132 results in a significant reduction in the synthesis of pre-tRNALeu by 72%, 80%, and 53% in actively proliferating cells of MG63, MDA361, and HEK293, respectively by inhibiting mTORC1. Moreover WYE-125132 is also found to industry the degradation of Maf1 (negative regulator of Pol III transcription) and its accumulation in the nucleus. WYE-125132 potently and competitively inhibits recombinant mTOR kinase by ATP with an IC50 of 0.19 nM and is more selective than acting on various PI3Ks and 230 protein kinase groups. In vitro, WYE-125132 exhibited significant anti-proliferative activity against a panel of tumor cell lines with IC50 ranging from 2 nM (LNCap) to 380 nM (HTC116). In addition, WYE-125132 also causes cell cycle progression, induction of apoptosis, and inhibition of protein synthesis and cell size. WYE-125132 causes pre-tRNA by inhibiting mTORC1 |
| In vivo study | WYE-125132 (5 mg/kg p.o.) products significant antitumor activity and causes dose-dependent tumor growth delay in the PI3K/mTOR- and HER2-hyperactive MDA361 tumor model. In addition, WYE-125132 also show strength antitumor efficacy in the PTEN-null glioma U87MG, non-small cell cancer H1975 and A549 models. In the MDA361 tumor model with PI3K/mTOR- and HER2-hyperactivity, WYE-125132 (5 mg/kg p.o.) this results in significant anti-tumor activity and a dose-dependent delay in tumor growth. In addition, WYE-125132 demonstrated potent anti-tumor activity in PTEN-deleted glioma U87MG, non-small cell lung cancer H1975 and A549 models. |
1144068-46-1 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.925 ml | 9.623 ml | 19.245 ml |
| 5 mM | 0.385 ml | 1.925 ml | 3.849 ml |
| 10 mM | 0.192 ml | 0.962 ml | 1.925 ml |
| 5 mM | 0.038 ml | 0.192 ml | 0.385 ml |
Last Update：2024-01-02 23:10:35
1144068-46-1 - Reference Information
| biological activity | WYE-125132 (WYE-132) is a highly effective, ATP-competitive mTOR inhibitor, IC50 is 0.19 nM; It is more selective to act on mTOR than on PI3Ks or PI3K-related kinases hSMG1 and ATR. WYE-125132 (WYE-132) is a highly effective, ATP-competitive mTOR inhibitor with IC50 as 0.19 nM. The selectivity of mTOR is higher than that of PI3Ks or PI3K related kinases hSMG1 and ATR. |
| in vitro study | WYE-125132 potently and ATP-competitively inhibits recombinant mTOR kinase with IC50 of 0.19 nM and also shows the high selectivity over various PI3Ks and a panel of 230 protein kinases. in vitro, WYE-125132 exhibits a significant anti-proliferative activity against a panel of tumor cell lines with ic50 ranging from 2 nm (lncap) to 380 nm (hc116). Besides, WYE-125132 also cause cell cycle progression, induction of apoptosis, and inhibition of protein synthesis and cell size. WYE-125132 results in a significant reduction in the synthesis of pre-tRNALeu by 72%, 80%, and 53% in actively proliferating cells of MG63, MDA361, and HEK293, respectively by inhibiting mTORC1. Moreover, WYE-125132 is also found to induce the dephosphorylation of Maf1 (negative regulator of Pol III transcription) and its accumulation in the nucleus. WYE-125132 is potent and ATP competitively inhibits recombinant mTOR kinase, IC50 is 0.19 nM, which is more selective than acting on various PI3Ks and 230 protein kinase groups. In vitro, WYE-125132 showed significant antiproliferative activity against a group of tumor cell lines, with IC50 ranging from 2 nM (LNCap) to 380 nM (HTC116). In addition, WYE-125132 can also cause cell cycle progression, apoptosis induction, and inhibition of protein synthesis and cell size. WYE-125132 causes pre-tRNA by inhibiting mTORC1 |
| in vivo study | WYE-125132 (5 mg/kg p.o.) produces significant antitumor activity and causes dose-dependent growth delay in the PI3K/mTOR- and HER2-hyperactive MDA361 tumor model. In addition, WYE-125132 also shows potent antitumor efficacy in the PTEN-null glioma U87MG, non-small cell lung cancer h1975 and a549 models. WYE-125132 (5 mg/kg p.o.) produces significant anti-tumor activity and causes dose-dependent delay of tumor growth in MDA361 tumor models with PI3K/mTOR- and HER2-extremely active. In addition, WYE-125132 exhibited potent antitumor activity in PTEN-deleted glioma U87MG, non-small cell lung cancer H1975 and A549 models. |
| features | WYE-125132 is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor. |
| target | TargetValue mTOR (Cell-free say) 0.19 nM |
| Target | Value |
| mTOR (Cell-free assay) | 0.19 nM |
Last Update：2024-04-09 21:54:55
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Product Name: WYE-125132 (WYE-132) Visit Supplier Webpage Request for quotationCAS: 1144068-46-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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