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| 化学名: | | | 英語化学名: | WP1066 | | 别名: | WP1066;(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide;WP1066/WP-1066;(S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide;(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide WP 1066;WP1066, >=99%;wp1066(STAT Inhibitor III);Stat3 Inhibitor III, WP1066 | | CAS番号: | 857064-38-1 | | 分子式: | C17H14BrN3O | | 分子量: | 356.22 | | EINECS: | | | カテゴリ情報: | Inhibitors;JAK;STAT;Inhibitor;API | | Mol File: | 857064-38-1.mol |  |
| 融点 | 90-93oC | | 沸点 | 569.9±50.0 °C(Predicted) | | 比重(密度) | 1.425 | | 貯蔵温度 | +2C to +8C | | 溶解性 | Soluble in DMSO (up to at least 25 mg/ml) | | 外見 | Off-white solid | | 酸解離定数(Pka) | 11.00±0.46(Predicted) | | 色 | White | | 安定性： | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| | WP1066 Usage And Synthesis |
| 説明 | WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells when given at a concentration of 10 μM. It also induces apoptosis in U87-MG (IC50 = 5.6 μM) and U373-MG (IC50 = 3.7 μM) cells. WP1066 is orally bioavailable, crosses the blood-brain barrier, and demonstrates in vivo activity, including immune activation as indicated by the up-regulation of CD80 and CD86 and the induction of proliferation of effector T cells. In addition to inducing apoptosis in cancer cells, WP1066 suppresses vascular smooth muscle cell proliferation after vascular injury in mice and prevents seizures following brain injury in rats. | | 使用 | WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells. | | target | JAK2 | | 参考文献 | 1) Kong?et al.?(2005),?Discovery of WP1066, a novel Stat3/c-myc inhibitor with potent antitumor activity against human melanoma in vitro and in vivo;?Cancer Res.?65?1387
2) Iwamaru?et al.?(2007),?A novel inhibitor of the STAT3 pathway induces apoptosis in malignant glioma cells both invitro and in vivo;?Oncogene?26?2435
3) Ferraioli?et al.?(2007),?WP1066 Disrupts Janus Kinase-2 and Induces Caspase-Dependent Apoptosis in acute Myelogenous Leukemia Cells;?Cancer Res.?67?11291
4) Kong,?et al.?(2008),?A novel inhibitor of signal transducers and activators of transcription 3 activation is efficacious against established central nervous system melanoma and inhibits regulatory T cells;?Clin. Cancer Res.?14?5759
5) Kong,?et al.?(2009),?A novel phosphorylated STAT3 inhibitor enhances T cell cytotoxicity against melanoma through inhibition of regulatory T cells;?Cancer Immunol. Immunother.?58?1023
6) Ma,?et al.?(2017),?Stat3 inhibitor abrogates the expression of PD-1 ligands on Lymphoma cell lines;?J. Clin. Exp. Hematop.?57?21 |
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