SB 590885

Catalog # Availability Size / Price Qty
2650/10
SB 590885 | CAS No. 405554-55-4 | Raf Kinase Inhibitors
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Description: Potent B-Raf inhibitor

Chemical Name: 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime

Purity: ≥98%

Product Details
Citations (3)
Reviews (1)

Biological Activity

SB 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.

Technical Data

M.Wt:
453.54
Formula:
C27H27N5O2
Solubility:
Soluble to 10 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
405554-55-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline.

Background References

  1. Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo.
    Najm F, Madhavan M, Zaremba A, Shick E, Karl R, Factor D, Miller T, Nevin Z, Kantor C, Sargent A, Quick K, Schlatzer D, Tang H, Papoian R, Brimacombe K, Shen M, Boxer M, Jadhav A, Robinson A, Podojil J, Miller S, Miller R, Tesar P
    Nature, 2015;522(7555):216-20.
  2. PRC2 specifies ectoderm lineages and maintains pluripotency in primed but not na�ve ESCs
    Y Shan, Z Liang, Q Xing, T Zhang, B Wang, S Tian, W Huang, Y Zhang, J Yao, Y Zhu, K Huang, Y Liu, X Wang, Q Chen, J Zhang, B Shang, S Li, X Shi, B Liao, C Zhang, K Lai, X Zhong, X Shu, J Wang, H Yao, J Chen, D Pei, G Pan
    Nat Commun, 2017;8(1):672.
  3. BMI1 enables interspecies chimerism with human pluripotent stem cells
    K Huang, Y Zhu, Y Ma, B Zhao, N Fan, Y Li, H Song, S Chu, Z Ouyang, Q Zhang, Q Xing, C Lai, N Li, T Zhang, J Gu, B Kang, Y Shan, K Lai, W Huang, Y Mai, Q Wang, J Li, A Lin, Y Zhang, X Zhong, B Liao, L Lai, J Chen, D Pei, G Pan
    Nat Commun, 2018;9(1):4649.
  4. Unique molecular events during reprogramming of human somatic cells to induced pluripotent stem cells (iPSCs) at na�ve state
    Y Wang, C Zhao, Z Hou, Y Yang, Y Bi, H Wang, Y Zhang, S Gao
    Elife, 2018;7(0):.
  5. Endophilin marks and controls a clathrin-independent endocytic pathway.
    Boucrot E, Ferreira A, Almeida-Souza L, Debard S, Vallis Y, Howard G, Bertot L, Sauvonnet N, McMahon H
    Nature, 2015;517(7535):460-5.
  6. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.
    King et al.
    Cancer Res., 2006;66:11100
  7. The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.
    Takle et al.
    Bioorg.Med.Chem.Lett., 2006;16:378
  8. Hominoid-Specific Transposable Elements and KZFPs Facilitate Human Embryonic Genome Activation and Control Transcription in Naive Human ESCs
    J Pontis, E Planet, S Offner, P Turelli, J Duc, A Coudray, TW Theunissen, R Jaenisch, D Trono
    Cell Stem Cell, 2019;0(0):.
  9. Capturing human trophoblast development with naive pluripotent stem cells in�vitro
    S Io, M Kabata, Y Iemura, K Semi, N Morone, A Minagawa, B Wang, I Okamoto, T Nakamura, Y Kojima, C Iwatani, H Tsuchiya, B Kaswandy, E Kondoh, S Kaneko, K Woltjen, M Saitou, T Yamamoto, M Mandai, Y Takashima
    Cell Stem Cell, 2021;28(6):1023-1039.e13.

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Citations for SB 590885

The citations listed below are publications that use Tocris products. Selected citations for SB 590885 include:

3 Citations: Showing 1 - 3

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Great effect
By Raj Kumar on 03/18/2021
Species: Human

Endothelial cells were subjected to pre-treatment with 0.05 micromole SB 590885 prior to FGF2 treatment, isolated protein, and immunoblotted for pMEK1 levels.


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