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Submit ReviewSB 590885 is a potent B-Raf inhibitor (Kd = 0.3 nM). Selective for B-Raf against 46 other kinases (Ki app values are 0.16 and 1.72 nM for B-Raf and c-Raf respectively). Decreases anchorage-independent growth of melanoma cell lines. Inhibits ERK phosphorylation and proliferation in tumor cells expressing B-RafV600E. The compound can be used in protocols for the chemical reprogramming of somatic cells to iPSCs.
Sold for research purposes under agreement from GlaxoSmithKline.
分子量 | 453.54 |
公式 | C27H27N5O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 405554-55-4 |
PubChem ID | 11316960 |
InChI Key | DPCXEUSDRQOOGZ-QLYXXIJNSA-N |
Smiles | CN(C)CCOC(C=C4)=CC=C4C1=NC(C3=CC=C(C(CC5)=NO)C5=C3)=C(C2=CC=NC=C2)N1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 4.54 | 10 |
以下数据基于产品分子量 453.54。 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 |
---|---|---|---|
0.1 mM | 22.05 mL | 110.24 mL | 220.49 mL |
0.5 mM | 4.41 mL | 22.05 mL | 44.1 mL |
1 mM | 2.2 mL | 11.02 mL | 22.05 mL |
5 mM | 0.44 mL | 2.2 mL | 4.41 mL |
参考文献是支持产品生物活性的出版物。
King et al (2006) Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res. 66 11100 PMID: 17145850
Takle et al (2006) The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg.Med.Chem.Lett. 16 378 PMID: 16260133
Guan et al (2022) Chemical reprogramming of human somatic cells to pluripotent stem cells. Nature 605 325 PMID: 35418683
If you know of a relevant reference for SB 590885, please let us know.
关键词: SB 590885, SB 590885 supplier, glaxosmithkline, SB590885, b-raf, braf, c-raf, kinases, inhibitors, inhibits, selective, induced, pluripotent, stem, cells, iPSC, reprogramming, Raf, Kinase, Stem, Cell, Reprogramming, 2650, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SB 590885 的部分引用包括:
Balaburski et al (2013) A modified HSP70 inhibitor shows broad activity as an anticancer agent. Mol Cancer Res 11 219 PMID: 23303345
Najm et al (2015) Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo. PLoS One 522 216 PMID: 25896324
Wagenaar et al (2014) Resistance to vemurafenib resulting from a novel mutation in the BRAFV600E kinase domain. Pigment Cell Melanoma Res 27 124 PMID: 24112705
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