Dabrafenib甲磺酸达拉非尼,1195768-06-9

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Dabrafenib Mesylate

CAS No. : 1195768-06-9

MCE 国际站：Dabrafenib Mesylate

产品活性：Dabrafenib Mesylate是ATP竞争型的 Raf 抑制剂，抑制 C-Raf 和 B-Raf^V600E 的 IC₅₀ 分别为 5 nM 和 0.6 nM。

研究领域：MAPK/ERK Pathway

作用靶点：Raf

In Vitro: Dabrafenib (GSK2118436, 1 μM) with 0.01 μM GSK1120212 inhibits more than 90% of cell growth in the NRAS mutant clones. GSK2118436 is sufficient to reduce S6P phosphorylation in A375. Dabrafenib suppresses the PolyP-mediated vascular barrier permeability, upregulation of inflammatory biomarkers, adhesion/migration of leukocytes, and activation and/or production of nuclear factor-κB, tumor necrosis factor-α, and interleukin-6. Dabrafenib inhibits the release of HMGB1 and downregulates HMGB1-dependent inflammatory responses by enhancing the expressions of cell adhesion molecules (CAMs) in human endothelial cells.

In Vivo: Dabrafenib-treated females have mostly immature reproductive tracts with no evidence of ovulation, similar to age-matched controls; however, DAB-treated females have keratinized and histologically open vaginas.

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