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Submit ReviewGalunisertib
说明： ALK4 and ALK5 (TGFβRI) inhibitor
别名： LY 2157299
化学名： 4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide
纯度： ≥98% (HPLC)
生物活性 for Galunisertib
Galunisertib is an ALK4 and ALK5 (TGFβRI) inhibitor (IC50 values are 77.7 and 172 nM, respectively). Also inhibits a range of other kinases with submicromolar IC50s including MINK, TGFβRII, ALK6 and ACVR2B. Inhibits TGFβ-induced SMAD phosphorylation in cancer cell lines in vitro and in vivo. Also reverses TGFβ-mediated suppression of T cell proliferation. Prevents TGFβ-mediated EMT and cell migration in vitro and exhibits antitumor efficacy in vivo. Used as component of growth media for urothelial organoids. Orally bioavailable.
化合物库 for Galunisertib
Galunisertib is also offered as part of the Tocriscreen Kinase Inhibitor Library and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Galunisertib
| 分子量 | 369.43 |
| 公式 | C22H19N5O |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 700874-72-2 |
| PubChem ID | 10090485 |
| InChI Key | IVRXNBXKWIJUQB-UHFFFAOYSA-N |
| Smiles | CC1=NC(C2=NN3CCCC3=C2C4=CC=NC5=C4C=C(C(N)=O)C=C5)=CC=C1 |
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 Galunisertib
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 36.94 | 100 | |
| ethanol | 7.39 | 20 |
制备储备液 for Galunisertib
以下数据基于产品分子量 369.43。 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 | 2.71 mL | 13.53 mL | 27.07 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.41 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.71 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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产品说明书 for Galunisertib
参考文献 for Galunisertib
参考文献是支持产品生物活性的出版物。
Yingling et al (2017) Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor. Oncotarget 9 6659 PMID: 29467918
Holmgaard et al (2018) Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete responses, as monotherapy and in combination with checkpoint blockade. J.Immunother.Cancer. 6 47 PMID: 29866156
Santos et al (2019) Urothelial organoids originating from Cd49fhigh mouse stem cells display Notch-dependent differentiation capacity. Nat.Commun. 10 4407 PMID: 31562298
If you know of a relevant reference for Galunisertib, please let us know.
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关键词: Galunisertib, Galunisertib supplier, TGFbetaRI, TGFBRI, inhibitors, inhibits, ALK5, ALK4, smad, phosphorylation, anticancer, orally, bioavailable, growth, media, organoids, LY, 2157299, TGF-beta, Receptors, Organoids, 6956, Tocris Bioscience
2 篇 Galunisertib 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Galunisertib 的部分引用包括：
David C et al (2020) A systems approach delivers a functional microRNA catalog and expanded targets for seizure suppression in temporal lobe epilepsy. Proc Natl Acad Sci U S A 117 15977-15988 PMID: 32581127
Natani et al (2022) Activation of TGF-β - SMAD2 signaling by IL-6 drives neuroendocrine differentiation of prostate cancer through p38MAPK. Cell Signal 91 110240 PMID: 34986386
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Galunisertib 的评论
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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。
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 Galunisertib
