Dabrafenib Mesylate|1195768-06-9|-陌孚医药/Medlife

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Dabrafenib Mesylate

目录号: PL10788 纯度: ≥99%

CAS No. :1195768-06-9

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中文名称	Dabrafenib Mesylate
中文别名	达拉菲尼甲磺酸盐;达拉芬尼甲磺酸盐;达帕菲尼甲磺酸盐;达拉非尼甲磺酸盐;Dabrafenib (Mesylate);甲磺酸达拉非尼
英文名称	Dabrafenib Mesylate
英文别名	Dabrafenib Mesylate(GSK-2118436B);Dabrafenib Mesylate;N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide,methanesulfonic acid;GSK 2118436B;GSK2118436 Mesylate;GSK-2118436 Mesylate;UNII-B6DC89I63E;GSK 2118436 methanesulfonate salt;N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoro-benzenesulfonamide methanesulfonate;Dabrafenib (Mesylate);METHANE SULFONATE SALT;Dabrafenib mesylate [USAN];B6DC89I63E;GSK2118436B;Dabrafenib mesylate (USAN);Taflinar;N-(3-(5-(2-aminopyrimidin-4-yl)-2-(tert-butyl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide methanesulfonate;Dabrafenib methanesulfonate;Tafinlar (TN);GSK2118436 Methane sulfonate salt
Cas No.	1195768-06-9
分子式	C₂₄H₂₄F₃N₅O₅S₃
分子量	615.67
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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。

生物活性

Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC 50 s of 0.6 and 5.0 nM for Raf and c-Raf, respectively.

性状

Solid

IC50 & Target[1][2]

BRaf 0.6 nM (IC50) CRAF 5 nM (IC50

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther, 2012, 11(4), 909-920.
[2]. Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22.

溶解度数据	In Vitro: DMSO : 20.83 mg/mL (33.83 mM; ultrasonic and warming and heat to 60°C)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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