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 克/摩尔
纯度
≥98%
产品说明书及文档
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相关材料与文献
技术资料 (2)
文献 (5)
Induction of functional islet-like cells from human iPS cells by suspension culture. Regenerative therapy 2019 jun
Abstract
Introduction To complement islet transplantation for type1 diabetic patients, cell-based therapy using pluripotent stem cells such as ES cells and iPS cells is promising. Many papers have already reported the induction of pancreatic $\beta$ cells from these cell types, but a suspension culture system has not usually been employed. The aim of this study is to establish a suspension culture method for inducing functional islet-like cells from human iPS cells. Methods We used 30 ml spinner type culture vessels for human iPS cells throughout the differentiation process. Differentiated cells were analyzed by immunostaining and C-peptide secretion. Cell transplantation experiments were performed with STZ-induced diabetic NOD/SCID mice. Blood human C-peptide and glucagon levels were measured serially in mice, and grafts were analyzed histologically. Results We obtained spherical pancreatic beta-like cells from human iPS cells and detected verifiable amounts of C-peptide secretion in vitro. We demonstrated reversal of hyperglycemia in diabetic model mice after transplantation of these cells, maintaining non-fasting blood glucose levels along with the human glycemic set point. We confirmed the secretion of human insulin and glucagon dependent on the blood glucose level in vivo. Immunohistological analysis revealed that grafted cells became $\alpha$, $\beta$ and $\delta$ cells in vivo. Conclusions These results suggest that differentiated cells derived from human iPS cells grown in suspension culture mature and function like pancreatic islets in vivo.
Axl inhibitor R428 induces apoptosis of cancer cells by blocking lysosomal acidification and recycling independent of Axl inhibition. American journal of cancer research 2018
Abstract
R428 (BGB324) is an anti-cancer drug candidate under clinical investigation. It inhibits the receptor tyrosine kinase Axl and induces apoptosis of many types of cancer cells, but the relationship between the two has not been well established. We investigated the molecular mechanisms of the R428-induced apoptosis and found that R428 induced extensive cytoplasmic vacuolization and caspase activation, independent of its inhibitory effects on Axl. Further analyses revealed that R428 blocked lysosomal acidification and recycling, accumulated autophagosomes and lysosomes, and induced cell apoptosis. Inhibition of autophagy by autophagy inhibitors or autophagic gene-knockout alleviated the R428-induced vacuoles formation and cell apoptosis. Our study uncovered a novel function and mechanism of R428 in addition to its ability to inhibit Axl. These data will help to better direct the application of R428 as an anti-cancer reagent. It also adds new knowledge to understand the regulation of autophagy and apoptosis.
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% |
