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GSK1838705A
点击次数：319发布时间：2013/4/3 16:05:59
更新日期：2022/8/19 17:45:40
所 在 地：美洲
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详细内容
GSK1838705A
上海义森生物科技有限公司
技术数据:
分子量（MW）: 532.57 
化学式: C27H29FN8O3
溶解度: DMSO 107mg/mL Water <1mg/mL Ethanol <1mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 1116235-97-2, 1116236-05-5 （H2O）
生物活性
GSK1838705A is a potent small-molecule IGF-IR, the insulin receptor ａnd anaplastic lymphoma kinase （ALK） inhibitor with IC50 of 2.0, 1.6 ａnd 0.5 nM, respectively. 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.[1]
技术数据:
分子量（MW）: 532.57 化学式: C27H29FN8O3
溶解度: DMSO 107mg/mL Water <1mg/mL Ethanol <1mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 1116235-97-2, 1116236-05-5 （H2O）
生物活性
GSK1838705A is a potent small-molecule IGF-IR, the insulin receptor ａnd anaplastic lymphoma kinase （ALK） inhibitor with IC50 of 2.0, 1.6 ａnd 0.5 nM, respectively. 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.[1]
技术数据:
分子量（MW）: 532.57 化学式: C27H29FN8O3
溶解度: DMSO 107mg/mL Water <1mg/mL Ethanol <1mg/mL 纯度: >99% 稳定性: at -20℃ 2 years CAS号: 1116235-97-2, 1116236-05-5 （H2O）
生物活性
GSK1838705A is a potent small-molecule IGF-IR, the insulin receptor ａnd anaplastic lymphoma kinase （ALK） inhibitor with IC50 of 2.0, 1.6 ａnd 0.5 nM, respectively. 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.[1]
技术数据:
| 分子量（MW）: | 532.57 | |
|---|---|---|
| 化学式: | C27H29FN8O3 | |
| 溶解度: | DMSO 107mg/mL Water <1mg/mL Ethanol <1mg/mL | |
| 纯度: | >99% | |
| 稳定性: | at -20℃ 2 years | |
| CAS号: | 1116235-97-2, 1116236-05-5 （H2O） |
生物活性
GSK1838705A is a potent small-molecule IGF-IR, the insulin receptor ａnd anaplastic lymphoma kinase （ALK） inhibitor with IC50 of 2.0, 1.6 ａnd 0.5 nM, respectively. 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.[1]
