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Submit ReviewGDC 0879
说明： Potent B-Raf inhibitor
化学名： 2,3-Dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-1H-inden-1-one oxime
纯度： ≥98% (HPLC)
生物活性 for GDC 0879
GDC 0879 is a potent and selective B-Raf inhibitor (IC50 = 0.13 nM against purified B-Raf V600E). Activity reduces phospho-ERK (pERK) levels (IC50 = 63 nM in the Malme-3M cell line). Inhibits the Raf/MEK/ERK signaling pathway in V600E B-Raf mutant cell lines. Does not activate apoptotic pathways in A375 or Colo205 cell lines. Orally bioavailable.
External Portal Information for GDC 0879
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GDC 0879 is reviewed on the chemical probes website.
化合物库 for GDC 0879
GDC 0879 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
技术数据 for GDC 0879
| 分子量 | 334.37 |
| 公式 | C19H18N4O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 905281-76-7 |
| PubChem ID | 11717001 |
| InChI Key | DEZZLWQELQORIU-RELWKKBWSA-N |
| Smiles | OCCN1N=C(C3=CC=NC=C3)C(C2=CC=C(/C(CC4)=N/O)C4=C2)=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 GDC 0879
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 33.44 | 100 |
制备储备液 for GDC 0879
以下数据基于产品分子量 334.37。 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 | 2.99 mL | 14.95 mL | 29.91 mL |
| 5 mM | 0.6 mL | 2.99 mL | 5.98 mL |
| 10 mM | 0.3 mL | 1.5 mL | 2.99 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
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产品说明书 for GDC 0879
参考文献 for GDC 0879
参考文献是支持产品生物活性的出版物。
Wong et al (2009) Pharmacodynamics of 2-{4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl}ethan-1-ol (GDC-0879), a potent and selective B-Raf kinase inhibitor: understanding relationships between systemic conc J.Pharmacol.Exp.Ther. 329 360 PMID: 19147858
Hatzivassiliou et al (2010) RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 464 431 PMID: 20130576
Hoeflich et al (2009) Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression. Cancer Res. 69 3042 PMID: 19276360
If you know of a relevant reference for GDC 0879, please let us know.
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关键词: GDC 0879, GDC 0879 supplier, GDC0879, b-raf, braf, inhibitors, inhibits, potent, selective, Raf, Kinase, 4453, Tocris Bioscience
1 篇 GDC 0879 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GDC 0879 的部分引用包括：
Konstantinos et al (2021) Cdk5 and GSK3β inhibit fast endophilin-mediated endocytosis. Nat Commun 12 2424 PMID: 33893293
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