使用 'B-Raf (V600E)' 作为标签的产品
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Raf 抑制剂
AZ628是一种RAF抑制剂,IC50值:BRAF V600E和野生型CRAF约为30 nM,野生型BRAF约为100 nM。
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Raf 抑制剂
Dabrafenib (GSK2118436A)是一种有效且选择性的B-RAF蛋白激酶抑制剂,具有V600E突变,目前正在临床试验中。
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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Chenyang He, .et al. Detection of Dabrafenib using Optical Fibre Long Period Grating Sensor Modified with Surface Imprinted Polymers for Dose Detection and Prevention of Cancer Resistance, Clinical and Translational Biophotonics, 2020, TTh3B.2
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Selective B-RAF 抑制剂
LGX 818 (Encorafenib)是一种Raf激酶抑制剂,具有潜在的抗肿瘤活性。
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- Seidel D, .et al. A multidimensional impedance platform for the real-time analysis of single and combination drug pharmacology in patient-derived viable melanoma models, Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
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Raf/MEK dual 抑制剂
RO5126766 (CH5126766)是对Raf和MEK丝裂原激活的蛋白激酶(MAPK)具有特异性的蛋白激酶抑制剂,具有潜在的抗肿瘤活性。
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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767