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Submit ReviewPotent, ATP-competitive Raf kinase inhibitor (IC50 = 10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively. Suppresses DNA synthesis and induces apoptosis in cells that proliferate in response to Raf-1 and A-Raf but not B-Raf.
分子量 | 347.8 |
公式 | C20H14ClN3O |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 303727-31-3 |
PubChem ID | 9950176 |
Smiles | ClC(C(O)=C4)=CC=C4C(N=C(C3=CC=CC=C3)N2)=C2C1=CC=NC=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.
参考文献是支持产品生物活性的出版物。
White (2003) Small-molecule inhibitors of signal transduction pathways in leukemia therapeutics: how to assess selectivity for malignant signals. Leukemia 17 1759 PMID: 12970775
Shelton et al (2003) Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation. Leukemia 17 1765 PMID: 12970777
Takle et al (2006) Identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg.Med.Chem.Letts. 16 378
Röring et al (2012) Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling. EMBO J. 31 2629 PMID: 22510884
关键词: L-779,450, L-779,450 supplier, Potent, raf, kinases, inhibitors, inhibits, a-raf, raf-1, L779450, Raf, Kinase, 3185, Tocris Bioscience
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