EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #100-0566_C
抑制受体酪氨酸激酶Axl
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总览
R428是一种强效的选择性Axl抑制剂（IC50 = 14 nM），具有抗增殖活性（Holland et al.）。Axl是一种受体酪氨酸激酶，参与细胞存活、增殖、粘附和迁移（Chen et al.）。R428与胰岛素受体、表皮生长因子受体、人表皮生长因子受体2和血小板源性生长因子受体β相比，对Axl的选择性高出100倍（Holland et al.）。
分化
·抑制脂肪前体细胞向成熟脂肪细胞分化（Lijnen et al.）。
·从人诱导性多能干细胞诱导β细胞成熟（Kushneret al.；Yabe et al.）。
癌症研究
·抑制Axl表达和乳腺癌细胞转移（Holland et al.）。
·阻断溶酶体酸化，诱导癌细胞凋亡（Chen et al.）。
别名
Bemcentinib; BGB 324
细胞类型
脂肪细胞，癌细胞及细胞系，胰腺细胞
应用
分化
研究领域
癌症
CAS 编号
1037624-75-1
化学式
C30H34N8
分子量
506.6 g/mol
纯度
≥98%
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
相关材料与文献
技术资料 (2)
文献 (5)
R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer.
Cancer research 2010 feb
Abstract
Accumulating evidence suggests important roles for the receptor tyrosine kinase Axl in cancer progression,invasion,metastasis,drug resistance,and patient mortality,highlighting Axl as an attractive target for therapeutic development. We have generated and characterized a potent and selective small-molecule inhibitor,R428,that blocks the catalytic and procancerous activities of Axl. R428 inhibits Axl with low nanomolar activity and blocked Axl-dependent events,including Akt phosphorylation,breast cancer cell invasion,and proinflammatory cytokine production. Pharmacologic investigations revealed favorable exposure after oral administration such that R428-treated tumors displayed a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. In support of an earlier study,R428 inhibited angiogenesis in corneal micropocket and tumor models. R428 administration reduced metastatic burden and extended survival in MDA-MB-231 intracardiac and 4T1 orthotopic (median survival,{\textgreater}80 days compared with 52 days; P {\textless} 0.05) mouse models of breast cancer metastasis. Additionally,R428 synergized with cisplatin to enhance suppression of liver micrometastasis. Our results show that Axl signaling regulates breast cancer metastasis at multiple levels in tumor cells and tumor stromal cells and that selective Axl blockade confers therapeutic value in prolonging survival of animals bearing metastatic tumors.
Growth arrest-specific protein 6 receptor antagonism impairs adipocyte differentiation and adipose tissue development in mice.
The Journal of pharmacology and experimental therapeutics 2011 may
Abstract
A low-molecular-weight receptor tyrosine kinase inhibitor,1-(6,7-dihydro-5H-benzo(6,7)cyclohepta(1,2-c)pyridazin-3-yl)-N3-((7-pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo(7)annulene-2-yl)-1H-1,2,4-triazole-3,5-diamine (R428) with high affinity and selectivity for the growth arrest-specific protein 6 (GAS6) receptor Axl was used to study a potential role of GAS6 signaling in adiposity. In vitro,R428 caused a concentration-dependent inhibition of preadipocyte differentiation into mature adipocytes,as evidenced by reduced lipid uptake. Inhibition of Axl-mediated signaling was confirmed by reduced levels of phospho-Akt activity. In vivo,oral administration of R428 for 5 weeks to mice kept on a high-fat diet resulted in significantly reduced weight gain and subcutaneous and gonadal fat mass. This was associated with marked adipocyte hypotrophy,enhanced macrophage infiltration,and apoptosis. Thus,affecting GAS6 signaling through receptor antagonism using a low-molecular-weight Axl antagonist impairs adipocyte differentiation and reduces adipose tissue development in a murine model of nutritionally induced obesity.
Stem cells to insulin secreting cells: two steps forward and now a time to pause?
Cell stem cell 2014 nov
Abstract
Two groups recently reported the in vitro differentiation of human embryonic stem cells into insulin-secreting cells,achieving an elusive goal for regenerative medicine. Herein we provide a perspective regarding these developments,compare phenotypes of the insulin-containing cells to human $\beta$ cells,and discuss implications for type 1 diabetes research and clinical care.
更多信息
| Molecular Weight | 506.6 g/mol |
|---|---|
| Alternative Names | Bemcentinib; BGB 324 |
| Cas Number | 1037624-75-1 |
| Chemical Formula | C30H34N8 |
| 纯度 | ≥ 98% |
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