GSK1838705A|1116235-97-2|-陌孚医药/Medlife

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GSK1838705A

目录号: PL03112 纯度: ≥98%

CAS No. :1116235-97-2

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中文名称	GSK1838705A
中文别名	2-[[2-[[1-[(二甲基氨基)乙酰基]-5-(甲氧基)-2,3-二氢-1H-吲哚-6-基]氨基]-7H-吡咯并[2,3-d]嘧啶-4-基]氨基]-6-氟-N-甲基苯甲酰胺;GSK1838705A 抑制剂
英文名称	GSK1838705A
英文别名	2-[[2-[[1-[(Dimethylamino)ethanoyl]-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide;GSK1838705A;2-[[2-[[1-[2-(dimethylamino)acetyl]-5-methoxy-2,3-dihydroindol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide;GSK 1838705;2-[(2-{[1-(N,N-dimethylglycyl)-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino}-1H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-6-fluoro-N-methylbenzamide;CS-0695;GSK-1838705A;pyrrolo[2,3-d]pyrimidine deriv.,40;2-[[2-[[1-[2-(Dimethylamino)acetyl]-2,3-dihydro-5-methoxy-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methyl-benzamide
Cas No.	1116235-97-2
分子式	C₂₇H₂₉N₈O₃F
分子量	532.57
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	GSK1838705A是高效，可逆的 IGF-IR 和胰岛素受体 (insulin receptor) 抑制剂，IC₅₀ 值分别为2.0 和 1.6 nM。也可抑制 ALK，IC₅₀ 值为0.5 nM。
生物活性	GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC 50 s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC 50 of 0.5 nM.
性状	Solid
IC50 & Target[1][2]	IC50: 2.0 nM (IGF-IR), 1.6 nM (insulin receptor), 0.5 nM (ALK)
体外研究(In Vitro)	In cellular phosphorylation assays, GSK1838705A potently inhibits IGF-IR and insulin receptor phosphorylation with IC50s of 85 and 79 nM, respectively. Ki values are 0.7 nM for IGF-IR and 1.1 nM for insulin receptor using the filter binding assay. GSK1838705A inhibits the proliferation in a panel of cell lines derived from solid and hematologic tumors. The EC50s of GSK1838705A range from 20 nM to >8 μM, but are <1 μM in most multiple myeloma and Ewings sarcoma cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	GSK1838705A shows robust antitumor activity in animal xenograft models. Tumor types likely to respond to GSK1838705A include multiple myeloma and Ewings sarcoma, as well as ALK-driven tumors (e.g., ALCL, NSCLC, and neuroblastoma). A single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg results in 35% and 65% inhibition of IGF-IR phosphorylation, respectively, whereas doses ≥1 mg/kg results in complete inhibition of ligand-induced IGF-IR phosphorylation. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (187.77 mM)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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