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GSK1838705A

GSK1838705A

品 牌 MCE
C A S 号 1116235-97-2
货 号 HY-13020
规 格 5mg
价 格(元) 1252.00
咨询优惠价
货号 规格 价格
HY-13020 5mg 1252.00
HY-13020 10mg 2325.00
HY-13020 50mg 6975.00
HY-13020 100mg 10114.00

产品说明


GSK1838705A是IGF-IR,InsR和ALK抑制剂,IC50分别为2.0,1.6和0.5 nM。



GSK1838705A的生物活性


GSK1838705A is a potent small-molecule IGF-1R, the insulin receptor and anaplastic lymphoma kinase (ALK) inhibitor with IC50 of 2.0, 1.6 and 0.5 nM, respectively.
IC50 value: 2.0/1.6/0.5 nM ( IGF-1R/InsR/ALK)
Target: IGF-1R/InsR/ALK
GSK1838705A prevents the in vitro proliferation of cell lines derived from solid and hematologic malignancies, including multiple myeloma and Ewing’s sarcoma, and retards the growth of human tumor xenografts in vivo. Despite the inhibitory effect of GSK1838705A on insulin receptor, minimal effects on glucose homeostasis were obtained at efficacious doses. A single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg led to 35% and 65% prevention of IGF-IR phosphorylation, respectively, whereas doses ≥1 mg/kg led to complete inhibition of ligand-induced IGF-IR phosphorylation. Meanwhile, at a dose of 30 mg/kg, prevention was lasted for ?24 hours after compound injection. GSK1838705A also suppresses the anaplastic lymphoma kinase (ALK), which mediates the aberrant growth of anaplastic large-cell lymphomas, some neuroblastomas, and a subset of non–small cell lung cancers. Due to its inhibition of ALK, GSK1838705A gives rise to complete regression of ALK-dependent tumors in vivo at well-tolerated doses.

化学信息


分子量 532.57 储存条件 参考CoA中推荐的条件进行储存。
分子式 C₂₇H₂₉FN₈O₃
CAS号 1116235-97-2
溶剂/溶解度 10 mM in DMSO

相关文献


[1]. Sabbatini P, et al. GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2009 Oct;8(10):2811-20.