Dabrafenib mesylate

Cat. No. 7223 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective B-Raf, CDK16 and NEK9 inhibitor; anticancer; also targets human proteins in the SARS-CoV-2 interactome

化学名： N-[3-[5-(2-Aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide methanesulfonate

纯度： ≥98% (HPLC)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for Dabrafenib mesylate

Dabrafenib mesylate is a potent and selective Raf kinase inhibitor (IC₅₀ values are 0.8, 3.2 and 5.0 nM for B-Raf^V600E, wild-type B-Raf and c-Raf, respectively). Exhibits selectivity for B-Raf over a panel of 270 other kinases. Arrests cell cycle in the G₁ phase and inhibits growth of B-Raf^V600E mutant melanoma and colon cancer cells in vitro and in vivo. Orally bioavailable. Also inhibits NEK9 (IC₅₀ <10 nM) and CDK16. Identified as targeting human host proteins that interact with SARS-CoV-2.

化合物库 for Dabrafenib mesylate

Dabrafenib mesylate is also offered as part of the Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。

技术数据 for Dabrafenib mesylate

分子量	615.66
公式	C₂₃H₂₀F₃N₅O₂S₂.CH₃SO₃H
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	1195768-06-9
PubChem ID	44516822
InChI Key	YKGMKSIHIVVYKY-UHFFFAOYSA-N
Smiles	CS(O)(=O)=O.CC(C)(C1=NC(C2=C(C(NS(=O)(C3=C(C=CC=C3F)F)=O)=CC=C2)F)=C(C4=NC(N)=NC=C4)S1)C

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.

溶解性数据 for Dabrafenib mesylate

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	30.78	50

制备储备液 for Dabrafenib mesylate

以下数据基于产品分子量 615.66。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
0.5 mM	3.25 mL	16.24 mL	32.49 mL
2.5 mM	0.65 mL	3.25 mL	6.5 mL
5 mM	0.32 mL	1.62 mL	3.25 mL
25 mM	0.06 mL	0.32 mL	0.65 mL

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产品说明书 for Dabrafenib mesylate

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Dabrafenib mesylate

参考文献是支持产品生物活性的出版物。

Phadke et al (2018) Dabrafenib inhibits the growth of BRAF-WT cancers through CDK16 and NEK9 inhibition. Mol.Oncol. 12 74 PMID: 29112787

Gordon et al (2020) A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. Nature 583 PMID: 32353859

Rheault et al (2013) Discovery of Dabrafenib: a selective inhibitor of Raf kinases with antitumor activity against B.Raf-driven tumors. ACS Med Chem Lett 4 358 PMID: 24900673

If you know of a relevant reference for Dabrafenib mesylate, please let us know.

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