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说明： Selective TGF-β kinase inhibitor
化学名： 4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]quinoline
纯度： ≥98% (HPLC)
生物活性 for LY 2109761
LY 2109761 is a selective dual TGF-β receptor type I and II (TβRI/II) inhibitor (Ki values are 38 and 300 nM in a cell-free assay, respectively); it inhibits the kinase activity of both TGF-βRI and TGF-βRII. In vitro, it significantly inhibits the growth, motility, and invasiveness of L3.6pl/GLT pancreatic cancer cells and completely suppresses TGF-β-induced Smad2 phosphorylation. In vivo, LY 2109761, in combination with Gemcitabine, significantly reduces tumor volume and spontaneous abdominal metastases in a murine model of metastatic pancreatic cancer. LY 2109761 is orally bioavailable.
技术数据 for LY 2109761
| 分子量 | 441.53 |
| 公式 | C26H27N5O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 700874-71-1 |
| PubChem ID | 11655119 |
| InChI Key | IHLVSLOZUHKNMQ-UHFFFAOYSA-N |
| Smiles | N1=CC=CC=C1C2=NN3C(=C2C=4C=CN=C5C=C(OCCN6CCOCC6)C=CC54)CCC3 |
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 LY 2109761
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 8.83 | 20 温和加热 | |
| ethanol | 8.83 | 20 温和加热 |
制备储备液 for LY 2109761
以下数据基于产品分子量 441.53。 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 |
|---|---|---|---|
| 0.2 mM | 11.32 mL | 56.62 mL | 113.24 mL |
| 1 mM | 2.26 mL | 11.32 mL | 22.65 mL |
| 2 mM | 1.13 mL | 5.66 mL | 11.32 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.26 mL |
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产品说明书 for LY 2109761
参考文献 for LY 2109761
参考文献是支持产品生物活性的出版物。
Melisi et al (2008) LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Mol.Cancer Ther. 7 829 PMID: 18413796
If you know of a relevant reference for LY 2109761, please let us know.
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关键词: LY 2109761, LY 2109761 supplier, LY2109761, selective, inhibitors, inhibits, TGF-βRI, TGF-βRII, TGF-β, TGF-betaRI, TGF-betaRII, TGFbRI, TGFbRII, TGFbR1, TGFbR2, tgf-b1, tgf-b2, transforming, growth, factors, beta, receptors, TGF-beta, in, vivo, orally, bioavailable, pancreatic, cancer, meta, Receptors, 7864, Tocris Bioscience
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该领域的文献
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Stem Cell Research Product Guide
This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:
- Self-renewal and Maintenance
- Differentiation
- Reprogramming
- Organoid Generation
- GMP and Ancillary Material Grade Products
Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.
Pathways for LY 2109761
