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Submit ReviewDeltarasin
说明： High affinity PDEδ-KRas interaction inhibitor; binds to PDEδ
化学名： 2-[4-[(2S)-2-(2-Phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole trihydrochloride
纯度： ≥99% (HPLC)
生物活性 for Deltarasin
Deltarasin is a high affinity PDEδ-KRAS interaction inhibitor (Kd = 41 nM); binds to PDEδ. Reduces proliferation and induces cell death of KRAS-dependent Panc-Tu-1 and Capan-1 pancreatic cancer cells. Attenuates tumor growth of Panc-Tu-1 xenografts in mice.
化合物库 for Deltarasin
Deltarasin is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Deltarasin
| 分子量 | 713.14 |
| 公式 | C40H37N5O.3HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1440898-82-7 |
| PubChem ID | 91826089 |
| InChI Key | NCIOVAYUMQEQEU-VKZSUDIWSA-N |
| Smiles | C12=CC=CC=C1N=C(C4=CC=C(OC[C@H]([C@H]8CCNCC8)N5C(C7=CC=CC=C7)=NC6=C5C=CC=C6)C=C4)N2CC3=CC=CC=C3.Cl.Cl.Cl |
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 Deltarasin
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 71.31 | 100 | |
| DMSO | 71.31 | 100 |
制备储备液 for Deltarasin
以下数据基于产品分子量 713.14。 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 | 1.4 mL | 7.01 mL | 14.02 mL |
| 5 mM | 0.28 mL | 1.4 mL | 2.8 mL |
| 10 mM | 0.14 mL | 0.7 mL | 1.4 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.28 mL |
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产品说明书 for Deltarasin
参考文献 for Deltarasin
参考文献是支持产品生物活性的出版物。
Zimmermann et al (2013) Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature 497 638 PMID: 23698361
Zimmermann et al (2014) Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site. J.Med.Chem. 57 5435 PMID: 24884780
If you know of a relevant reference for Deltarasin, please let us know.
关键词: Deltarasin, Deltarasin supplier, high, affinity, PDEdelta, PDED, PDEδ, PDE6D, phosphodiesterases, KRAS, inhibitors, inhibits, Phosphodiesterases, Ras, GTPases, 5424, Tocris Bioscience
2 篇 Deltarasin 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Deltarasin 的部分引用包括：
Rudolf A et al (2022) An In Vivo Inflammatory Loop Potentiates KRAS Blockade. Biomedicines 10 PMID: 35327394
Malcolm G et al (2022) RNA splicing is a key mediator of tumour cell plasticity and a therapeutic vulnerability in colorectal cancer. Nat Commun 13 2791 PMID: 35589755
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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。
Cancer Metabolism Research Product Guide
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
- Glycolysis
- Tricarboxylic Acid Cycle
- Lipidogenesis
- 1C Metabolism and Nucleic Acid Synthesis
- Drivers of Metabolic Reprogramming
- pH and Redox Balance
RAS Oncoproteins Scientific Review
Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. 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.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Pathways for Deltarasin
Akt Signaling Pathway
The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.