GSK 1838705

Cat. No. 5111 1 次引用提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent IR and IGF1R inhibitor; also inhibits anaplastic lymphoma kinase (ALK)

化学名： 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

纯度： ≥98% (HPLC)

引用文献 (1)

文献 (2)

通路 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for GSK 1838705

GSK 1838705 is a potent insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) inhibitor (IC₅₀ values are 1.6 and 2 nM, respectively). Also inhibits anaplastic lymphoma kinase (ALK) (IC₅₀ = 0.5 nM). Displays > 800-fold selectivity for IR, IGFR1 and ALK over a panel of 44 kinases including JNK. Blocks proliferation of cancer cell lines in vitro, and causes complete regression of ALK-dependent tumors in vivo. Orally bioavailable.

许可信息

Sold for research purposes under agreement from GlaxoSmithKline.

化合物库 for GSK 1838705

GSK 1838705 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for GSK 1838705

分子量	532.57
公式	C₂₇H₂₉FN₈O₃
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	1116235-97-2
PubChem ID	25182616
InChI Key	HZTYDQRUAWIZRE-UHFFFAOYSA-N
Smiles	O=C(CN(C)C)N4CCC(C4=C5)=CC(OC)=C5NC1=NC(NC3=C(C(NC)=O)C(F)=CC=C3)=C2C(NC=C2)=N1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for GSK 1838705

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	53.26	100

制备储备液 for GSK 1838705

以下数据基于产品分子量 532.57。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	1.88 mL	9.39 mL	18.78 mL
5 mM	0.38 mL	1.88 mL	3.76 mL
10 mM	0.19 mL	0.94 mL	1.88 mL
50 mM	0.04 mL	0.19 mL	0.38 mL

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产品说明书 for GSK 1838705

分析证书/产品说明书

化学品安全技术说明书

参考文献 for GSK 1838705

参考文献是支持产品生物活性的出版物。

Sabbatini et al (2009) GSK1838705A inhibits the Ins-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol.Cancer.Ther. 8 2811 PMID: 19825801

Gao et al (2014) Site-specific activation of AKT protects cells from death induced by glucose deprivation. Oncogene 33 745 PMID: 23396361

Chamberlain et al (2009) Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg.Med.Chem.Lett. 19 360 PMID: 19071018

If you know of a relevant reference for GSK 1838705, please let us know.

按标靶查看相关产品

关键词: GSK 1838705, GSK 1838705 supplier, GSK1838705, potent, and, selective, IR, IGF1R, inhibitors, inhibits, antitumor, insulin, receptor, like, growth, factor, 1, anaplastic, lymphoma, kinase, ALK, Insulin, Insulin-like, Receptors, insulin-like, 5111, Tocris Bioscience

1 篇 GSK 1838705 的引用文献

引用文献是使用了 Tocris 产品的出版物。 GSK 1838705 的部分引用包括：

William B et al (2017) Insulin fine-tunes self-renewal pathways governing naive pluripotency and extra-embryonic endoderm. Nat Cell Biol 19 1164-1177 PMID: 28945231

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Pathways for GSK 1838705

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.