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Merck
CN
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主要文件

安全信息

SML0995

Sigma-Aldrich

GSK1838705A

≥98% (HPLC)

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, 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

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About This Item

经验公式（希尔记法）:
C27H29FN8O3
CAS号:
1116235-97-2
分子量:
532.57
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to light brown

溶解性

DMSO: 20 mg/mL, clear

储存温度

−20°C

SMILES字符串

Fc1c(c(ccc1)Nc2nc(nc5[nH]ccc52)Nc3cc4c(cc3OC)CCN4C(=O)CN(C)C)C(=O)NC

InChI

1S/C27H29FN8O3/c1-29-26(38)23-17(28)6-5-7-18(23)31-25-16-8-10-30-24(16)33-27(34-25)32-19-13-20-15(12-21(19)39-4)9-11-36(20)22(37)14-35(2)3/h5-8,10,12-13H,9,11,14H2,1-4H3,(H,29,38)(H3,30,31,32,33,34)

InChI key

HZTYDQRUAWIZRE-UHFFFAOYSA-N

应用

GSK1838705A has been used as an insulin receptor inhibitor in Roswell Park memorial institute medium (RPMI) 1640 medium for inhibitor experiments, to prove that the induction of interleukin-1 β (IL-1β) is dependent on insulin receptor signaling.

生化/生理作用

GSK1838705A can be used to treat prostate cancer (PC). It is capable of decreasing the viability of docetaxel-sensitive and docetaxel-resistant prostate cancer cells. GSK1838705A can stimulate apoptosis of PC-3R cells. It is an alternative therapeutic option for crizotinib-resistant anaplastic large cell lymphoma (ALCL).
GSK1838705A is a cell penetrant anti-tumor agent that potently inhibits the insulin-like growth factor-I receptors (IGF-IR), insulin receptors (IR) and anaplastic lymphoma kinase (ALK). GSK1838705A potently inhibits cell proliferation of multiple solid and hematologic cancers and retards the growth of human tumor xenografts. GSK1838705A does not significantly affect other kinases. GSK1838705A has minimal effects on glucose homeostasis in mice.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number
0000405532
0000405534
0000405532
0000405534
0000217953

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Julia Manowsky et al.
American journal of physiology. Endocrinology and metabolism, 310(11), E938-E946 (2016-04-21)
Overweight and obesity are associated with hyperinsulinemia, insulin resistance, and a low-grade inflammation. Although hyperinsulinemia is generally thought to result from an attempt of the β-cell to compensate for insulin resistance, there is evidence that hyperinsulinaemia itself may contribute to
GSK1838705a, an IGF-1R/ALK Inhibitor, Overcomes Resistance to Crizotinib in ALK-Positive ALCL
Shi, Wenyu and Li, Jian-Yong
Blood (2019)
GSK1838705a, an IGF-1R/ALK Inhibitor, Overcomes Resistance to Crizotinib in ALK-Positive ALCL
Shi, Wenyu and Li, Jian-Yong
Blood (2019)
Fayou Zhou et al.
OncoTargets and therapy, 8, 753-760 (2015-05-01)
Prostate cancer is the leading malignancy and the second most common cause of cancer-related death in men. Despite high cure rates with surgery and/or radiation, 30%-40% of patients eventually develop advanced cancer. Docetaxel is one of the most effective and
Natalia J Sumi et al.
Cell chemical biology, 26(9), 1240-1252 (2019-07-02)
Despite recent successes of precision and immunotherapies there is a persisting need for novel targeted or multi-targeted approaches in complex diseases. Through a systems pharmacology approach, including phenotypic screening, chemical and phosphoproteomics, and RNA-seq, we elucidated the targets and mechanisms

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