Linsitinib

Cat. No. 7652 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 and selective dual inhibitor of the IGF-1 receptor and insulin receptor

化学名： cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol

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 Linsitinib

Linsitinib is a potent and selective dual inhibitor of the IGF-1 receptor (IC₅₀ = 35 nM) and insulin receptor (IC₅₀= 75 nM); it inhibits ligand-dependent auto-phosphorylation of both receptor tyrosine kinases and prevents ligand-induced activation of downstream pathways including pAKT, pERK1/2 and p-p70S6K. The compound is selective for IGF-1R, IR and IRR in a panel of 88 kinases. Lisintinib inhibits proliferation in a variety of tumor cell lines and shows robust in vivo antitumor efficacy in an IGF-1R-driven LSN xenograft model. Orally bioavailable.

化合物库 for Linsitinib

Linsitinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for Linsitinib

分子量	421.49
公式	C₂₆H₂₃N₅O
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	867160-71-2
PubChem ID	11640390
InChI Key	PKCDDUHJAFVJJB-VLZXCDOPNA-N
Smiles	NC=1C=2N(C(=NC2C3=CC4=C(C=C3)C=CC(=N4)C5=CC=CC=C5)[C@]6(C[C@@](C)(O)C6)[H])C=CN1

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 Linsitinib

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	42.15	100

制备储备液 for Linsitinib

以下数据基于产品分子量 421.49。 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	2.37 mL	11.86 mL	23.73 mL
5 mM	0.47 mL	2.37 mL	4.75 mL
10 mM	0.24 mL	1.19 mL	2.37 mL
50 mM	0.05 mL	0.24 mL	0.47 mL

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产品说明书 for Linsitinib

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Linsitinib

参考文献是支持产品生物活性的出版物。

Mulvihill et al (2009) Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med.Chem. 1 1153 PMID: 21425998

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

按标靶查看相关产品

关键词: Linsitinib, Linsitinib supplier, potent, selective, inhibitors, inhibits, IGF-1, receptors, insulin-like, anti-tumor, growth, factor, Insulin, and, Receptors, 7652, Tocris Bioscience

1 篇 Linsitinib 的引用文献

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

Meier et al (2023) Epicardioid single-cell genomics uncovers principles of human epicardium biology in heart development and disease. Nat Biotechnol PMID: 37012447

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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for Linsitinib

Insulin Signaling Pathway

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