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说明： Potent pan-TEAD inhibitor
化学名： N-[(1S)-1-(2-Pyridinyl)ethyl]-5-[4-(trifluoromethyl)phenyl]-2-naphthalenecarboxamide
纯度： ≥98% (HPLC)
生物活性 for VT 104
VT 104 is a potent pan-TEAD (transcriptional enhanced associate domain) inhibitor (IC50 = 10.4 nM). VT 104 inhibits YAP/TAZ-TEAD promoted gene transcription by preventing the association between YAP/TAZ and TEAD. VT 104 blocks TEAD auto-palmitoylation. In vitro, VT 104 inhibits NF2-deficient mesothelioma cell proliferation, and growth of subcutaneous tumor xenografts in vivo. VT 104 is orally bioavailable.
技术数据 for VT 104
| 分子量 | 420.43 |
| 公式 | C25H19F3N2O |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2417718-25-1 |
| PubChem ID | 146909371 |
| InChI Key | AAZUPSFRSHFTGV-INIZCTEOSA-N |
| Smiles | C(N[C@@H](C)C1=CC=CC=N1)(=O)C2=CC3=C(C(=CC=C3)C4=CC=C(C(F)(F)F)C=C4)C=C2 |
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 VT 104
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 42.04 | 100 | |
| ethanol | 21.02 | 50 |
制备储备液 for VT 104
以下数据基于产品分子量 420.43。 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 | 2.38 mL | 11.89 mL | 23.79 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.76 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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产品说明书 for VT 104
参考文献 for VT 104
参考文献是支持产品生物活性的出版物。
Tang et al (2021) Small molecule inhibitors of TEAD auto-palmitoylation selectively inhibit proliferation and tumor growth of NF2-deficient mesothelioma. Mol.Cancer Ther. 20 986 PMID: 33850002
If you know of a relevant reference for VT 104, please let us know.
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关键词: VT 104, VT 104 supplier, VT104, VT-104, inhibitors, inhibits, potent, orally, bioavailable, in, vivo, YAP, TAZ, transcription, factor, TEAD, cell, antiproliferation, cancer, TEA, domain, palmitoylation, hippo, Hippo/Yap, signaling, Other, Transcription, Factors, 8176, Tocris Bioscience
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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 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.
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
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 VT 104
MAPK Signaling Pathway
The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.
Notch Signaling Pathway
The Notch pathway is involved in determination of cell fate, regulation of pattern formation and other developmental settings. Disrupted signaling can cause developmental defects and a range of adult pathologies.